| Year |
Citation |
Score |
| 2024 |
Dötsch L, Davies C, Hennes E, Schönfeld J, Kumar A, Guita CDCL, Ehrler JHM, Hiesinger K, Thavam S, Janning P, Sievers S, Knapp S, Proschak E, Ziegler S, Waldmann H. Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator. Journal of Medicinal Chemistry. 67: 4691-4706. PMID 38470246 DOI: 10.1021/acs.jmedchem.3c02245 |
0.312 |
|
| 2024 |
Schweipert M, Nehls T, Frühauf A, Debarnot C, Kumar A, Knapp S, Lermyte F, Meyer-Almes FJ. The catalytic domain of free or ligand bound histone deacetylase 4 occurs in solution predominantly in closed conformation. Protein Science : a Publication of the Protein Society. 33: e4917. PMID 38358265 DOI: 10.1002/pro.4917 |
0.312 |
|
| 2024 |
Bauer N, Balourdas DI, Schneider JR, Zhang X, Berger LM, Berger BT, Schwalm MP, Klopp NA, Siveke JT, Knapp S, Joerger AC. Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization. Acs Chemical Biology. PMID 38291964 DOI: 10.1021/acschembio.3c00427 |
0.357 |
|
| 2023 |
Amrhein JA, Berger LM, Balourdas DI, Joerger AC, Menge A, Krämer A, Frischkorn JM, Berger BT, Elson L, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T. Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3. Journal of Medicinal Chemistry. PMID 38126712 DOI: 10.1021/acs.jmedchem.3c01980 |
0.377 |
|
| 2023 |
Outhwaite IR, Singh S, Berger BT, Knapp S, Chodera JD, Seeliger MA. Death by a thousand cuts through kinase inhibitor combinations that maximize selectivity and enable rational multitargeting. Elife. 12. PMID 38047771 DOI: 10.7554/eLife.86189 |
0.399 |
|
| 2023 |
Sanz Murillo M, Villagran Suarez A, Dederer V, Chatterjee D, Alegrio Louro J, Knapp S, Mathea S, Leschziner AE. Inhibition of Parkinson's disease-related LRRK2 by type I and type II kinase inhibitors: Activity and structures. Science Advances. 9: eadk6191. PMID 38039358 DOI: 10.1126/sciadv.adk6191 |
0.312 |
|
| 2023 |
Tiek D, Wells CI, Schröder M, Song X, Alamillo-Ferrer C, Goenka A, Iglesia R, Lu M, Hu B, Kwarcinski F, Sintha P, de Silva C, Hossain MA, Picado A, Zuercher W, ... ... Knapp S, et al. SGC-CLK-1: A chemical probe for the Cdc2-like kinases CLK1, CLK2, and CLK4. Current Research in Chemical Biology. 3. PMID 38009092 DOI: 10.1016/j.crchbi.2023.100045 |
0.394 |
|
| 2023 |
Chauhan C, Kraemer A, Knapp S, Windheim M, Kotlyarov A, Menon MB, Gaestel M. 5-Iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFκB signaling. Cell Death Discovery. 9: 262. PMID 37495567 DOI: 10.1038/s41420-023-01576-x |
0.339 |
|
| 2023 |
Deau E, Lindberg MF, Miege F, Roche D, George N, George P, Krämer A, Knapp S, Meijer L. Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B. Journal of Medicinal Chemistry. PMID 37487467 DOI: 10.1021/acs.jmedchem.3c00884 |
0.346 |
|
| 2023 |
Amrhein JA, Wang G, Berger BT, Berger LM, Kalampaliki AD, Krämer A, Knapp S, Hanke T. Design and Synthesis of Pyrazole-Based Macrocyclic Kinase Inhibitors Targeting BMPR2. Acs Medicinal Chemistry Letters. 14: 833-840. PMID 37312836 DOI: 10.1021/acsmedchemlett.3c00127 |
0.302 |
|
| 2023 |
Choi JY, Noguchi Y, Alburger JM, Bayle S, Chung E, Grant W, Chaikuad A, Knapp S, Duckett DR, Roush WR. Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ. Journal of Medicinal Chemistry. PMID 37204207 DOI: 10.1021/acs.jmedchem.2c01180 |
0.381 |
|
| 2023 |
Rak M, Tesch R, Berger LM, Shevchenko E, Raab M, Tjaden A, Zhubi R, Balourdas DI, Joerger AC, Poso A, Krämer A, Elson L, Lučić A, Kronenberger T, Hanke T, ... ... Knapp S, et al. Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily. European Journal of Medicinal Chemistry. 254: 115347. PMID 37094449 DOI: 10.1016/j.ejmech.2023.115347 |
0.374 |
|
| 2023 |
Arora R, Linders JTM, Aci-Sèche S, Verheyen T, Van Heerde E, Brehmer D, Chaikuad A, Knapp S, Bonnet P. Design, synthesis and characterisation of a novel type II B-RAF paradox breaker inhibitor. European Journal of Medicinal Chemistry. 250: 115231. PMID 36878151 DOI: 10.1016/j.ejmech.2023.115231 |
0.349 |
|
| 2023 |
Schwalm MP, Knapp S, Rogov VV. Toward effective Atg8-based ATTECs: Approaches and perspectives. Journal of Cellular Biochemistry. PMID 36780422 DOI: 10.1002/jcb.30380 |
0.362 |
|
| 2023 |
Outhwaite IR, Singh S, Berger BT, Knapp S, Chodera JD, Seeliger MA. Death by a Thousand Cuts â€" Combining Kinase Inhibitors for Selective Target Inhibition and Rational Polypharmacology. Biorxiv : the Preprint Server For Biology. PMID 36711619 DOI: 10.1101/2023.01.13.523972 |
0.401 |
|
| 2023 |
Ali MM, Naz S, Ashraf S, Knapp S, Ul-Haq Z. Epigenetic modulation by targeting bromodomain containing protein 9 (BRD9): Its therapeutic potential and selective inhibition. International Journal of Biological Macromolecules. 123428. PMID 36709803 DOI: 10.1016/j.ijbiomac.2023.123428 |
0.369 |
|
| 2023 |
Němec V, Khirsariya P, Janovská P, Moyano PM, Maier L, Lesáková P, Kebková P, Gybel' T, Berger BT, Chaikuad A, Reinecke M, Küster B, Knapp S, Bryja V, Paruch K. Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity. Angewandte Chemie (International Ed. in English). PMID 36625768 DOI: 10.1002/anie.202217532 |
0.385 |
|
| 2022 |
Schröder M, Leiendecker M, Grädler U, Braun J, Blum A, Wanior M, Berger BT, Krämer A, Müller S, Esdar C, Knapp S, Heinrich T. MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core. Journal of Medicinal Chemistry. PMID 36516476 DOI: 10.1021/acs.jmedchem.2c01705 |
0.401 |
|
| 2022 |
Amrhein JA, Berger LM, Tjaden A, Krämer A, Elson L, Tolvanen T, Martinez-Molina D, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T. Discovery of 3-Amino-1-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family. International Journal of Molecular Sciences. 23. PMID 36499165 DOI: 10.3390/ijms232314834 |
0.36 |
|
| 2022 |
Laux J, Forster M, Riexinger L, Schwamborn A, Guezguez J, Pokoj C, Kudolo M, Berger LM, Knapp S, Schollmeyer D, Guse J, Burnet M, Laufer SA. Pharmacokinetic Optimization of Small Molecule Janus Kinase 3 Inhibitors to Target Immune Cells. Acs Pharmacology & Translational Science. 5: 573-602. PMID 35983274 DOI: 10.1021/acsptsci.2c00054 |
0.319 |
|
| 2022 |
Schwalm MP, Berger LM, Meuter MN, Vasta JD, Corona CR, Röhm S, Berger BT, Farges F, Beinert SM, Preuss F, Morasch V, Rogov VV, Mathea S, Saxena K, Robers MB, ... ... Knapp S, et al. A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins. Frontiers in Cell and Developmental Biology. 10: 886537. PMID 35721509 DOI: 10.3389/fcell.2022.886537 |
0.386 |
|
| 2022 |
Strubel A, Münick P, Chaikuad A, Dreier B, Schaefer J, Gebel J, Osterburg C, Tuppi M, Schäfer B, Knapp S, Plückthun A, Dötsch V. Designed Ankyrin Repeat Proteins as a tool box for analyzing p63. Cell Death and Differentiation. PMID 35717504 DOI: 10.1038/s41418-022-01030-y |
0.302 |
|
| 2022 |
Kurz CG, Preuss F, Tjaden A, Cusack M, Amrhein JA, Chatterjee D, Mathea S, Berger LM, Berger BT, Krämer A, Weller M, Weiss T, Müller S, Knapp S, Hanke T. Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-]pyrimidine-Based Macrocycles. Journal of Medicinal Chemistry. PMID 35608370 DOI: 10.1021/acs.jmedchem.2c00173 |
0.348 |
|
| 2022 |
Preuss F, Chatterjee D, Dederer V, Knapp S, Mathea S. Enabling pseudokinases as potential drug targets. Methods in Enzymology. 667: 663-683. PMID 35525558 DOI: 10.1016/bs.mie.2022.03.050 |
0.396 |
|
| 2022 |
Schwalm MP, Knapp S. BET bromodomain inhibitors. Current Opinion in Chemical Biology. 68: 102148. PMID 35462054 DOI: 10.1016/j.cbpa.2022.102148 |
0.381 |
|
| 2022 |
Zeinyeh W, Esvan YJ, Josselin B, Defois M, Baratte B, Knapp S, Chaikuad A, Anizon F, Giraud F, Ruchaud S, Moreau P. Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. European Journal of Medicinal Chemistry. 236: 114369. PMID 35447555 DOI: 10.1016/j.ejmech.2022.114369 |
0.402 |
|
| 2022 |
Dimitrov T, Anli C, Moschopoulou AA, Kronenberger T, Kudolo M, Geibel C, Schwalm MP, Knapp S, Zender L, Forster M, Laufer S. Development of novel urea-based ATM kinase inhibitors with subnanomolar cellular potency and high kinome selectivity. European Journal of Medicinal Chemistry. 235: 114234. PMID 35325634 DOI: 10.1016/j.ejmech.2022.114234 |
0.42 |
|
| 2022 |
Bonagas N, Gustafsson NMS, Henriksson M, Marttila P, Gustafsson R, Wiita E, Borhade S, Green AC, Vallin KSA, Sarno A, Svensson R, Göktürk C, Pham T, Jemth AS, Loseva O, ... ... Knapp S, et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nature Cancer. 3: 156-172. PMID 35228749 DOI: 10.1038/s43018-022-00331-y |
0.348 |
|
| 2022 |
Singh RK, Soliman A, Guaitoli G, Störmer E, von Zweydorf F, Dal Maso T, Oun A, Van Rillaer L, Schmidt SH, Chatterjee D, David JA, Pardon E, Schwartz TU, Knapp S, Kennedy EJ, et al. Nanobodies as allosteric modulators of Parkinson's disease-associated LRRK2. Proceedings of the National Academy of Sciences of the United States of America. 119. PMID 35217606 DOI: 10.1073/pnas.2112712119 |
0.337 |
|
| 2022 |
M Serafim RA, da Silva Santiago A, Schwalm MP, Hu Z, Dos Reis CV, Takarada JE, Mezzomo P, Massirer KB, Kudolo M, Gerstenecker S, Chaikuad A, Zender L, Knapp S, Laufer S, Couñago RM, et al. Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. Journal of Medicinal Chemistry. 65: 3173-3192. PMID 35167750 DOI: 10.1021/acs.jmedchem.1c01165 |
0.388 |
|
| 2022 |
Chatterjee D, Preuss F, Dederer V, Knapp S, Mathea S. Structural Aspects of LIMK Regulation and Pharmacology. Cells. 11. PMID 35011704 DOI: 10.3390/cells11010142 |
0.328 |
|
| 2021 |
Luciano V, Proschak E, Langer JD, Knapp S, Heering J, Marschalek R. Closantel is an allosteric inhibitor of human Taspase1. Iscience. 24: 103524. PMID 34934933 DOI: 10.1016/j.isci.2021.103524 |
0.4 |
|
| 2021 |
Bata N, Chaikuad A, Bakas NA, Limpert AS, Lambert LJ, Sheffler DJ, Berger LM, Liu G, Yuan C, Wang L, Peng Y, Dong J, Celeridad M, Layng F, Knapp S, et al. Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia. Journal of Medicinal Chemistry. PMID 34807584 DOI: 10.1021/acs.jmedchem.1c00804 |
0.359 |
|
| 2021 |
Gerstenecker S, Haarer L, Schröder M, Kudolo M, Schwalm MP, Wydra V, Serafim RAM, Chaikuad A, Knapp S, Laufer S, Gehringer M. Discovery of a Potent and Highly Isoform-Selective Inhibitor of the Neglected Ribosomal Protein S6 Kinase Beta 2 (S6K2). Cancers. 13. PMID 34680283 DOI: 10.3390/cancers13205133 |
0.367 |
|
| 2021 |
Russ N, Schröder M, Berger BT, Mandel S, Aydogan Y, Mauer S, Pohl C, Drewry DH, Chaikuad A, Müller S, Knapp S. Design and Development of a Chemical Probe for Pseudokinase Ca/calmodulin-Dependent Ser/Thr Kinase. Journal of Medicinal Chemistry. PMID 34543009 DOI: 10.1021/acs.jmedchem.1c00845 |
0.33 |
|
| 2021 |
Röhm S, Berger BT, Schröder M, Chatterjee D, Mathea S, Joerger AC, Pinkas DM, Bufton JC, Tjaden A, Kovooru L, Kudolo M, Pohl C, Bullock AN, Müller S, Laufer S, ... Knapp S, et al. Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe. Journal of Medicinal Chemistry. PMID 34506142 DOI: 10.1021/acs.jmedchem.1c00868 |
0.366 |
|
| 2021 |
Serafim RAM, Sorrell FJ, Berger BT, Collins RJ, Vasconcelos SNS, Massirer KB, Knapp S, Bennett J, Fedorov O, Patel H, Zuercher WJ, Elkins JM. Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold. Journal of Medicinal Chemistry. PMID 34463505 DOI: 10.1021/acs.jmedchem.0c01579 |
0.432 |
|
| 2021 |
Attwood MM, Fabbro D, Sokolov AV, Knapp S, Schiöth HB. Trends in kinase drug discovery: targets, indications and inhibitor design. Nature Reviews. Drug Discovery. PMID 34354255 DOI: 10.1038/s41573-021-00252-y |
0.354 |
|
| 2021 |
Nonga OE, Lavogina D, Enkvist E, Kestav K, Chaikuad A, Dixon-Clarke SE, Bullock AN, Kopanchuk S, Ivan T, Ekambaram R, Viht K, Knapp S, Uri A. Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules (Basel, Switzerland). 26. PMID 34299628 DOI: 10.3390/molecules26144353 |
0.347 |
|
| 2021 |
Mathea S, Salah E, Tallant C, Chatterjee D, Berger BT, Konietzny R, Müller-Knapp S, Kessler BM, Knapp S. Conformational plasticity of the ULK3 kinase domain. The Biochemical Journal. PMID 34190988 DOI: 10.1042/BCJ20210257 |
0.534 |
|
| 2021 |
Tesch R, Rak M, Raab M, Berger LM, Kronenberger T, Joerger AC, Berger BT, Abdi I, Hanke T, Poso A, Strebhardt K, Sanhaji M, Knapp S. Structure-Based Design of Selective Salt-Inducible Kinase Inhibitors. Journal of Medicinal Chemistry. PMID 34086472 DOI: 10.1021/acs.jmedchem.0c02144 |
0.347 |
|
| 2021 |
Reynders M, Chaikuad A, Berger BT, Bauer K, Koch P, Laufer S, Knapp S, Trauner D. Controlling the Covalent Reactivity of a Kinase Inhibitor with Light. Angewandte Chemie (International Ed. in English). PMID 34081840 DOI: 10.1002/anie.202103767 |
0.346 |
|
| 2021 |
Dölle A, Adhikari B, Krämer A, Weckesser J, Berner N, Berger LM, Diebold M, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Gebel J, Löhr F, Dötsch V, Eilers M, Heinzlmeir S, ... ... Knapp S, et al. Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders. Journal of Medicinal Chemistry. PMID 33980013 DOI: 10.1021/acs.jmedchem.1c00146 |
0.317 |
|
| 2021 |
Ni X, Schröder M, Olieric V, Sharpe ME, Hernandez-Olmos V, Proschak E, Merk D, Knapp S, Chaikuad A. Structural Insights into Plasticity and Discovery of Remdesivir Metabolite GS-441524 Binding in SARS-CoV-2 Macrodomain. Acs Medicinal Chemistry Letters. 12: 603-609. PMID 33850605 DOI: 10.1021/acsmedchemlett.0c00684 |
0.378 |
|
| 2021 |
Karatas M, Chaikuad A, Berger B, Kubbutat MHG, Totzke F, Knapp S, Kunick C. 7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones Designed by a "Cut and Glue" Strategy Are Dual Aurora A/VEGF-R Kinase Inhibitors. Molecules (Basel, Switzerland). 26. PMID 33799460 DOI: 10.3390/molecules26061611 |
0.37 |
|
| 2021 |
Hartmann M, Huber J, Kramer JS, Heering J, Pietsch L, Stark H, Odadzic D, Bischoff I, Fürst R, Schröder M, Akutsu M, Chaikuad A, Dötsch V, Knapp S, Biondi RM, et al. Demonstrating Ligandability of the LC3A and LC3B Adapter Interface. Journal of Medicinal Chemistry. PMID 33769048 DOI: 10.1021/acs.jmedchem.0c01564 |
0.334 |
|
| 2021 |
Berger BT, Amaral M, Kokh DB, Nunes-Alves A, Musil D, Heinrich T, Schröder M, Neil R, Wang J, Navratilova I, Bomke J, Elkins JM, Müller S, Frech M, Wade RC, ... Knapp S, et al. Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2. Cell Chemical Biology. PMID 33497606 DOI: 10.1016/j.chembiol.2021.01.003 |
0.371 |
|
| 2021 |
Wells CI, Drewry DH, Pickett JE, Tjaden A, Krämer A, Müller S, Gyenis L, Menyhart D, Litchfield DW, Knapp S, Axtman AD. Development of a potent and selective chemical probe for the pleiotropic kinase CK2. Cell Chemical Biology. PMID 33484635 DOI: 10.1016/j.chembiol.2020.12.013 |
0.354 |
|
| 2021 |
Malik AU, Karapetsas A, Nirujogi RS, Mathea S, Chatterjee D, Pal P, Lis P, Taylor M, Purlyte E, Gourlay R, Dorward M, Weidlich S, Toth R, Polinski NK, Knapp S, et al. Deciphering the LRRK code: LRRK1 and LRRK2 phosphorylate distinct Rab proteins and are regulated by diverse mechanisms. The Biochemical Journal. PMID 33459343 DOI: 10.1042/BCJ20200937 |
0.301 |
|
| 2021 |
Harrington L, Alexander LT, Knapp S, Bayley H. Nanopore Enzymology to Study Protein Kinases and Their Inhibition by Small Molecules. Methods in Molecular Biology (Clifton, N.J.). 2186: 95-114. PMID 32918732 DOI: 10.1007/978-1-0716-0806-7_8 |
0.347 |
|
| 2020 |
Wurzlbauer A, Rüben K, Gürdal E, Chaikuad A, Knapp S, Sippl W, Becker W, Bracher F. How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition-The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine. Molecules (Basel, Switzerland). 25. PMID 33339338 DOI: 10.3390/molecules25245962 |
0.348 |
|
| 2020 |
Forster M, Liang XJ, Schröder M, Gerstenecker S, Chaikuad A, Knapp S, Laufer S, Gehringer M. Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK. International Journal of Molecular Sciences. 21. PMID 33291717 DOI: 10.3390/ijms21239269 |
0.399 |
|
| 2020 |
Wanior M, Preuss F, Ni X, Krämer A, Mathea S, Göbel T, Heidenreich D, Simonyi S, Kahnt AS, Joerger AC, Knapp S. Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis. Journal of Medicinal Chemistry. PMID 33216538 DOI: 10.1021/acs.jmedchem.0c01242 |
0.316 |
|
| 2020 |
Picado A, Chaikuad A, Wells CI, Shrestha S, Zuercher WJ, Pickett JE, Kwarcinski FE, Sinha P, de Silva CS, Zutshi R, Liu S, Kannan N, Knapp S, Drewry DH, Willson TM. A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation. Journal of Medicinal Chemistry. PMID 33215924 DOI: 10.1021/acs.jmedchem.0c01174 |
0.326 |
|
| 2020 |
Ren H, Bakas NA, Vamos M, Chaikuad A, Limpert AS, Wimer CD, Brun SN, Lambert LJ, Tautz L, Celeridad M, Sheffler DJ, Knapp S, Shaw RJ, Cosford NDP. Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry. PMID 33200929 DOI: 10.1021/acs.jmedchem.0c00873 |
0.357 |
|
| 2020 |
Quevedo CE, Bataille CJR, Byrne S, Durbin M, Elkins J, Guillermo A, Jones AM, Knapp S, Nadali A, Walker RG, Wilkinson IVL, Wynne GM, Davies SG, Russell AJ. Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family. Bioorganic & Medicinal Chemistry. 28: 115724. PMID 33128909 DOI: 10.1016/J.Bmc.2020.115724 |
0.393 |
|
| 2020 |
Schröder M, Filippakopoulos P, Schwalm MP, Ferrer CA, Drewry DH, Knapp S, Chaikuad A. Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3. International Journal of Molecular Sciences. 21. PMID 33114754 DOI: 10.3390/ijms21217953 |
0.398 |
|
| 2020 |
Elie J, Feizbakhsh O, Desban N, Josselin B, Baratte B, Bescond A, Duez J, Fant X, Bach S, Marie D, Place M, Ben Salah S, Chartier A, Berteina-Raboin S, Chaikuad A, ... Knapp S, et al. Design of new disubstituted imidazo[1,2-]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation. Journal of Enzyme Inhibition and Medicinal Chemistry. 35: 1840-1853. PMID 33040634 DOI: 10.1080/14756366.2020.1825408 |
0.378 |
|
| 2020 |
Röhm S, Schröder M, Dwyer JE, Widdowson CS, Chaikuad A, Berger BT, Joerger AC, Krämer A, Harbig J, Dauch D, Kudolo M, Laufer S, Bagley MC, Knapp S. Selective targeting of the αC and DFG-out pocket in p38 MAPK. European Journal of Medicinal Chemistry. 208: 112721. PMID 33035818 DOI: 10.1016/J.Ejmech.2020.112721 |
0.346 |
|
| 2020 |
Juettner NE, Bogen JP, Bauer TA, Knapp S, Pfeifer F, Huettenhain SH, Meusinger R, Kraemer A, Fuchsbauer HL. Decoding the Papain Inhibitor from as Being Hydroxylated Chymostatin Derivatives: Purification, Structure Analysis, and Putative Biosynthetic Pathway. Journal of Natural Products. PMID 32998509 DOI: 10.1021/acs.jnatprod.0c00201 |
0.303 |
|
| 2020 |
Adhikari B, Bozilovic J, Diebold M, Schwarz JD, Hofstetter J, Schröder M, Wanior M, Narain A, Vogt M, Dudvarski Stankovic N, Baluapuri A, Schönemann L, Eing L, Bhandare P, Kuster B, ... ... Knapp S, et al. PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase. Nature Chemical Biology. PMID 32989298 DOI: 10.1038/s41589-020-00652-y |
0.378 |
|
| 2020 |
Krämer A, Kurz CG, Berger BT, Celik IE, Tjaden A, Greco FA, Knapp S, Hanke T. Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. European Journal of Medicinal Chemistry. 208: 112770. PMID 32883634 DOI: 10.1016/j.ejmech.2020.112770 |
0.35 |
|
| 2020 |
Preuss F, Chatterjee D, Mathea S, Shrestha S, St-Germain J, Saha M, Kannan N, Raught B, Rottapel R, Knapp S. Nucleotide Binding, Evolutionary Insights, and Interaction Partners of the Pseudokinase Unc-51-like Kinase 4. Structure (London, England : 1993). PMID 32814032 DOI: 10.1016/J.Str.2020.07.016 |
0.337 |
|
| 2020 |
Schröder M, Bullock AN, Fedorov O, Bracher F, Chaikuad A, Knapp S. DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity. Journal of Medicinal Chemistry. PMID 32787076 DOI: 10.1021/acs.jmedchem.0c00898 |
0.379 |
|
| 2020 |
Schröder M, Tan L, Wang J, Liang Y, Gray NS, Knapp S, Chaikuad A. Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities. Cell Chemical Biology. PMID 32783966 DOI: 10.1016/J.Chembiol.2020.07.014 |
0.36 |
|
| 2020 |
Sheetz JB, Mathea S, Karvonen H, Malhotra K, Chatterjee D, Niininen W, Perttilä R, Preuss F, Suresh K, Stayrook SE, Tsutsui Y, Radhakrishnan R, Ungureanu D, Knapp S, Lemmon MA. Structural Insights into Pseudokinase Domains of Receptor Tyrosine Kinases. Molecular Cell. PMID 32619402 DOI: 10.1016/J.Molcel.2020.06.018 |
0.339 |
|
| 2020 |
Zhang X, Zegar T, Weiser T, Hamdan FH, Berger BT, Lucas R, Balourdas DI, Ladigan S, Cheung PF, Liffers ST, Trajkovic-Arsic M, Scheffler B, Joerger AC, Hahn SA, Johnsen SA, ... Knapp S, et al. Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinoma. International Journal of Cancer. PMID 32599645 DOI: 10.1002/ijc.33137 |
0.37 |
|
| 2020 |
Galvez Bulh Otilde Es Pedreira JUL, Nahidino P, Kudolo M, Pantsar T, Berger BT, Forster M, Knapp S, Laufer SA, Barreiro EJ. Bioisosteric Replacement of Arylamide-linked Spine Residues by N-Acylhydrazones and Selenophenes as Design Strategy to Novel Dibenzosuberone Derivatives as Type I½ p38 MAP Kinase Inhibitors. Journal of Medicinal Chemistry. PMID 32462866 DOI: 10.1021/Acs.Jmedchem.0C00508 |
0.302 |
|
| 2020 |
Zhang X, Zegar T, Lucas A, Morrison-Smith C, Knox T, French CA, Knapp S, Müller S, Siveke JT. Therapeutic targeting of p300/CBP HAT domain for the treatment of NUT midline carcinoma. Oncogene. PMID 32366905 DOI: 10.1038/s41388-020-1301-9 |
0.37 |
|
| 2020 |
Hanke T, Wong JF, Berger BT, Abdi I, Berger LM, Tesch R, Tredup C, Bullock AN, Müller-Knapp S, Knapp S. A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5. Acs Chemical Biology. PMID 32176847 DOI: 10.1021/acschembio.0c00076 |
0.323 |
|
| 2020 |
Merdanovic M, Burston SG, Schmitz AL, Köcher S, Knapp S, Clausen T, Kaiser M, Huber R, Ehrmann M. Activation by substoichiometric inhibition. Proceedings of the National Academy of Sciences of the United States of America. PMID 31907318 DOI: 10.1073/Pnas.1918721117 |
0.4 |
|
| 2019 |
Ni X, Heidenreich D, Christott T, Bennett J, Moustakim M, Brennan PE, Fedorov O, Knapp S, Chaikuad A. Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1. Acs Medicinal Chemistry Letters. 10: 1661-1666. PMID 31857843 DOI: 10.1021/Acsmedchemlett.9B00460 |
0.306 |
|
| 2019 |
Lechner C, Flaßhoff M, Falke H, Preu L, Loaëc N, Meijer L, Knapp S, Chaikuad A, Kunick C. []-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors. Molecules (Basel, Switzerland). 24. PMID 31766108 DOI: 10.3390/molecules24224090 |
0.388 |
|
| 2019 |
Röhm S, Berger BT, Schröder M, Chaikuad A, Winkel R, Hekking KFW, Benningshof JJC, Mueller G, Tesch R, Kudolo M, Forster M, Laufer SA, Knapp S. A fast iterative synthetic approach towards the identification of novel highly selective p38 MAP kinase inhibitors. Journal of Medicinal Chemistry. PMID 31702918 DOI: 10.1021/Acs.Jmedchem.9B01227 |
0.369 |
|
| 2019 |
Salah E, Chatterjee D, Beltrami A, Tumber A, Preuss F, Canning P, Chaikuad A, Knaus P, Knapp S, Bullock AN, Mathea S. Lessons from LIMK1 enzymology and their impact on inhibitor design. The Biochemical Journal. PMID 31652302 DOI: 10.1042/BCJ20190517 |
0.393 |
|
| 2019 |
Kramer JS, Woltersdorf S, Duflot T, Hiesinger K, Lillich FF, Knöll F, Wittmann SK, Klingler FM, Brunst S, Chaikuad A, Morisseau C, Hammock BD, Buccellati C, Sala A, Rovati GE, ... ... Knapp S, et al. Discovery of first in vivo active inhibitors of soluble epoxide hydrolase (sEH) phosphatase domain. Journal of Medicinal Chemistry. PMID 31436984 DOI: 10.1021/Acs.Jmedchem.9B00445 |
0.323 |
|
| 2019 |
Wu Q, Heidenreich D, Zhou S, Ackloo S, Krämer A, Nakka K, Lima-Fernandes E, Deblois G, Duan S, Vellanki RN, Li F, Vedadi M, Dilworth J, Lupien M, Brennan PE, ... ... Knapp S, et al. A chemical toolbox for the study of bromodomains and epigenetic signaling. Nature Communications. 10: 1915. PMID 31015424 DOI: 10.1038/S41467-019-09672-2 |
0.338 |
|
| 2019 |
Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Li T, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, et al. Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome. Cell Chemical Biology. PMID 30982749 DOI: 10.1016/J.Chembiol.2019.02.021 |
0.374 |
|
| 2019 |
Watts E, Heidenreich D, Tucker E, Raab M, Strebhardt K, Chesler L, Knapp S, Bellenie B, Hoelder S. Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. Journal of Medicinal Chemistry. PMID 30789735 DOI: 10.1021/Acs.Jmedchem.8B01947 |
0.347 |
|
| 2019 |
Chaikuad A, Koschade SE, Stolz A, Zivkovic K, Pohl C, Shaid S, Ren H, Lambert LJ, Cosford NDP, Brandts CH, Knapp S. Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2). The Biochemical Journal. PMID 30782972 DOI: 10.1042/Bcj20190038 |
0.428 |
|
| 2019 |
Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry D, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, et al. SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK). Journal of Medicinal Chemistry. PMID 30768268 DOI: 10.1021/acs.jmedchem.8b01213 |
0.356 |
|
| 2019 |
Tazarki H, Zeinyeh W, Esvan YJ, Knapp S, Chatterjee D, Schröder M, Joerger AC, Khiari J, Josselin B, Baratte B, Bach S, Ruchaud S, Anizon F, Giraud F, Moreau P. New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis. European Journal of Medicinal Chemistry. 166: 304-317. PMID 30731399 DOI: 10.1016/j.ejmech.2019.01.052 |
0.321 |
|
| 2018 |
D'Ascenzio M, Pugh KM, Konietzny R, Berridge G, Tallant C, Hashem S, Monteiro O, Thomas JR, Schirle M, Knapp S, Marsden B, Fedorov O, Bountra C, Kessler BM, Brennan PE. An Activity-Based Probe Targeting Non-Catalytic, Highly Conserved Amino Acid Residues within Bromodomains. Angewandte Chemie (International Ed. in English). PMID 30589164 DOI: 10.1002/Anie.201807825 |
0.561 |
|
| 2018 |
Němec V, Hylsová M, Maier L, Flegel J, Sievers S, Ziegler S, Schroeder M, Berger BT, Chaikuad A, Valčíková B, Uldrijan S, Drápela S, Souček K, Waldmann H, Knapp S, et al. Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway. Angewandte Chemie (International Ed. in English). PMID 30569600 DOI: 10.1002/anie.201810312 |
0.316 |
|
| 2018 |
Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Saez LD, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, ... ... Knapp S, et al. Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angewandte Chemie (International Ed. in English). PMID 30288907 DOI: 10.1002/Anie.201810617 |
0.376 |
|
| 2018 |
Carlson DA, Singer MR, Sutherland C, Redondo C, Alexander LT, Hughes PF, Knapp S, Gurley SB, Sparks MA, MacDonald JA, Haystead TAJ. Targeting Pim Kinases and DAPK3 to Control Hypertension. Cell Chemical Biology. PMID 30033129 DOI: 10.1016/J.Chembiol.2018.06.006 |
0.304 |
|
| 2018 |
Forster M, Chaikuad A, Dimitrov T, Döring E, Holstein J, Berger BT, Gehringer M, Ghoreschi K, Müller S, Knapp S, Laufer SA. Development, Optimization and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4-d]pyrrolo[2,3-b]pyridine Scaffold. Journal of Medicinal Chemistry. PMID 29852068 DOI: 10.1021/Acs.Jmedchem.8B00571 |
0.389 |
|
| 2018 |
Walter A, Chaikuad A, Helmer R, Loaëc N, Preu L, Ott I, Knapp S, Meijer L, Kunick C. Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype. Plos One. 13: e0196761. PMID 29723265 DOI: 10.1371/journal.pone.0196761 |
0.35 |
|
| 2018 |
Heroven C, Georgi V, Ganotra GK, Brennan PE, Wolfreys F, Wade RC, Fernández-Montalván AE, Chaikuad A, Knapp S. Halogen-aromatic π-interactions modulate inhibitor residence time. Angewandte Chemie (International Ed. in English). PMID 29601130 DOI: 10.1002/Anie.201801666 |
0.328 |
|
| 2018 |
Moustakim M, Riedel K, Schuller M, Gehring AP, Monteiro OP, Martin SP, Fedorov O, Heer J, Dixon DJ, Elkins JM, Knapp S, Bracher F, Brennan PE. Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2. Bioorganic & Medicinal Chemistry. PMID 29567296 DOI: 10.1016/J.Bmc.2018.03.020 |
0.671 |
|
| 2017 |
Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, ... ... Knapp S, et al. Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. Cell Chemical Biology. PMID 29174542 DOI: 10.1016/j.chembiol.2017.10.010 |
0.366 |
|
| 2017 |
Chaikuad A, Koch P, Laufer S, Knapp S. Targeting the Protein Kinases Cysteinome. Angewandte Chemie (International Ed. in English). PMID 28994500 DOI: 10.1002/anie.201707875 |
0.344 |
|
| 2017 |
Schuller M, Riedel K, Gibbs-Seymour I, Uth K, Sieg C, Gehring AP, Ahel I, Bracher F, Kessler BM, Elkins JM, Knapp S. Discovery of a selective allosteric inhibitor targeting macrodomain 2 of poly-adenosine-diphosphate-ribose polymerases 14. Acs Chemical Biology. PMID 28991428 DOI: 10.1021/Acschembio.7B00445 |
0.677 |
|
| 2017 |
Ferguson FM, Doctor ZM, Chaikuad A, Sim T, Kim ND, Knapp S, Gray NS. Characterization of a highly selective inhibitor of the Aurora kinases. Bioorganic & Medicinal Chemistry Letters. PMID 28818446 DOI: 10.1016/J.Bmcl.2017.08.016 |
0.397 |
|
| 2017 |
Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, et al. Progress towards a public chemogenomic set for protein kinases and a call for contributions. Plos One. 12: e0181585. PMID 28767711 DOI: 10.1371/Journal.Pone.0181585 |
0.332 |
|
| 2017 |
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, ... Knapp S, et al. Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins. Journal of Medicinal Chemistry. PMID 28714688 DOI: 10.1021/Acs.Jmedchem.7B00611 |
0.327 |
|
| 2017 |
Melo-Hanchuk TD, Slepicka PF, Meirelles GV, Basei FL, Lovato DV, Granato DC, Pauletti BA, Domingues RR, Leme AFP, Pelegrini AL, Lenz G, Knapp S, Elkins JM, Kobarg J. NEK1 kinase domain structure and its dynamic protein interactome after exposure to Cisplatin. Scientific Reports. 7: 5445. PMID 28710492 DOI: 10.1038/S41598-017-05325-W |
0.309 |
|
| 2017 |
Bataille CJ, Brennan MB, Byrne S, Davies SG, Durbin M, Fedorov O, Huber KV, Jones AM, Knapp S, Liu G, Nadali A, Quevedo CE, Russell AJ, Walker RG, Westwood R, et al. Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family. Bioorganic & Medicinal Chemistry. PMID 28341403 DOI: 10.1016/J.Bmc.2017.02.056 |
0.342 |
|
| 2017 |
Batson J, Toop HD, Redondo C, Babaei-Jadidi R, Chaikuad A, Wearmouth SF, Gibbons B, Allen C, Tallant C, Zhang J, Du C, Hancox J, Hawtrey T, Da Rocha J, Griffith R, ... Knapp S, et al. Development of potent, selective SRPK1 inhibitors as potential topical therapeutics for neovascular eye disease. Acs Chemical Biology. PMID 28135068 DOI: 10.1021/Acschembio.6B01048 |
0.352 |
|
| 2016 |
Walter A, Chaikuad A, Loaëc N, Preu L, Knapp S, Meijer L, Kunick C, Koch O. Identification of CLK1 Inhibitors by a Fragment-linking Based Virtual Screening. Molecular Informatics. PMID 28000414 DOI: 10.1002/minf.201600123 |
0.44 |
|
| 2016 |
Navratilova I, Aristotelous T, Picaud S, Chaikuad A, Knapp S, Filappakopoulos P, Hopkins AL. Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening. Acs Medicinal Chemistry Letters. 7: 1213-1218. PMID 27994766 DOI: 10.1021/acsmedchemlett.6b00154 |
0.324 |
|
| 2016 |
Olzscha H, Fedorov O, Kessler BM, Knapp S, La Thangue NB. CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation. Cell Chemical Biology. PMID 27989401 DOI: 10.1016/j.chembiol.2016.11.009 |
0.474 |
|
| 2016 |
Lu M, Breyssens H, Salter V, Zhong S, Hu Y, Baer C, Ratnayaka I, Sullivan A, Brown NR, Endicott J, Knapp S, Kessler BM, Middleton MR, Siebold C, Jones EY, et al. Restoring p53 Function in Human Melanoma Cells by Inhibiting MDM2 and Cyclin B1/CDK1-Phosphorylated Nuclear iASPP. Cancer Cell. 30: 822-823. PMID 27846394 DOI: 10.1016/j.ccell.2016.09.019 |
0.457 |
|
| 2016 |
Forster M, Chaikuad A, Bauer SM, Holstein J, Robers MB, Corona CR, Gehringer M, Pfaffenrot E, Ghoreschi K, Knapp S, Laufer SA. Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket. Cell Chemical Biology. PMID 27840070 DOI: 10.1016/j.chembiol.2016.10.008 |
0.419 |
|
| 2016 |
Chaikuad A, Diharce J, Schröder M, Foucourt A, Leblond B, Casagrande AS, Desire L, Bonnet P, Knapp S, Besson T. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-specificity Tyrosine Phosphorylation-Regulated Kinases. Journal of Medicinal Chemistry. PMID 27766861 DOI: 10.1021/acs.jmedchem.6b01083 |
0.367 |
|
| 2016 |
Picaud S, Leonards K, Lambert JP, Dovey O, Wells C, Fedorov O, Monteiro O, Fujisawa T, Wang CY, Lingard H, Tallant C, Nikbin N, Guetzoyan L, Ingham R, Ley SV, ... ... Knapp S, et al. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia. Science Advances. 2: e1600760. PMID 27757418 DOI: 10.1126/Sciadv.1600760 |
0.377 |
|
| 2016 |
Ma Y, Wang L, Neitzel LR, Loganathan S, Tang N, Qin L, Emily CE, Guo Y, Knapp S, Beauchamp RD, Lee E, Wang J. The MAPK pathway regulates intrinsic resistance to BET inhibitors in colorectal cancer. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. PMID 27678457 DOI: 10.1158/1078-0432.Ccr-16-0453 |
0.313 |
|
| 2016 |
Popp TA, Tallant C, Rogers C, Fedorov O, Brennan PE, Müller S, Knapp S, Bracher F. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. Journal of Medicinal Chemistry. PMID 27673482 DOI: 10.1021/Acs.Jmedchem.6B00774 |
0.407 |
|
| 2016 |
Miranda F, Mannion D, Liu S, Zheng Y, Mangala LS, Redondo C, Herrero-Gonzalez S, Xu R, Taylor C, Chedom DF, Karaminejadranjbar M, Albukhari A, Jiang D, Pradeep S, Rodriguez-Aguayo C, ... ... Knapp S, et al. Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche. Cancer Cell. PMID 27478041 DOI: 10.1016/J.Ccell.2016.06.020 |
0.459 |
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| 2016 |
Lori L, Pasquo A, Lori C, Petrosino M, Chiaraluce R, Tallant C, Knapp S, Consalvi V. Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability. Plos One. 11: e0159180. PMID 27403962 DOI: 10.1371/journal.pone.0159180 |
0.34 |
|
| 2016 |
Milhas S, Raux B, Betzi S, Derviaux C, Roche P, Restouin A, Basse MJ, Rebuffet E, Lugari A, Badol M, Kashyap R, Lissitzky JC, Eydoux C, Hamon V, Gourdel ME, ... ... Knapp S, et al. Protein-protein interaction inhibition (2P2I)-oriented chemical library accelerates hit discovery. Acs Chemical Biology. PMID 27219844 DOI: 10.1021/acschembio.6b00286 |
0.307 |
|
| 2016 |
Sdelci S, Lardeau CH, Tallant C, Klepsch F, Klaiber B, Bennett J, Rathert P, Schuster M, Penz T, Fedorov O, Superti-Furga G, Bock C, Zuber J, Huber KV, Knapp S, et al. Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. Nature Chemical Biology. PMID 27159579 DOI: 10.1038/Nchembio.2080 |
0.379 |
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| 2016 |
Lavogina D, Kestav K, Chaikuad A, Heroven C, Knapp S, Uri A. Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors. Acta Crystallographica. Section F, Structural Biology Communications. 72: 339-45. PMID 27139824 DOI: 10.1107/S2053230X16004611 |
0.408 |
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| 2016 |
Esvan YJ, Zeinyeh W, Boibessot T, Nauton L, Théry V, Knapp S, Chaikuad A, Loaëc N, Meijer L, Anizon F, Giraud F, Moreau P. Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure. European Journal of Medicinal Chemistry. 118: 170-177. PMID 27128181 DOI: 10.1016/j.ejmech.2016.04.004 |
0.307 |
|
| 2016 |
Sutherell CL, Tallant C, Monteiro OP, Yapp C, Fuchs JE, Fedorov O, Siejka P, Müller S, Knapp S, Brenton JD, Brennan PE, Ley SV. Identification and development of 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one inhibitors targeting bromodomains within the Switch/Sucrose Non-Fermenting complex. Journal of Medicinal Chemistry. PMID 27119626 DOI: 10.1021/Acs.Jmedchem.5B01997 |
0.332 |
|
| 2016 |
Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers CM, Parikh MD, Taylor A, Samas BM, O'Mahony A, Berg EL, ... ... Knapp S, et al. Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit. Journal of Medicinal Chemistry. PMID 27115555 DOI: 10.1021/Acs.Jmedchem.6B00012 |
0.314 |
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| 2016 |
Mathea S, Abdul Azeez KR, Salah E, Tallant C, Wolfreys F, Konietzny R, Fischer R, Lou HJ, Brennan PE, Schnapp G, Pautsch A, Kessler BM, Turk BE, Knapp S. Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib. Acs Chemical Biology. PMID 26999302 DOI: 10.1021/Acschembio.6B00043 |
0.588 |
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| 2016 |
Ghari F, Quirke AM, Munro S, Kawalkowska J, Picaud S, McGouran J, Subramanian V, Muth A, Williams R, Kessler B, Thompson PR, Fillipakopoulos P, Knapp S, Venables PJ, La Thangue NB. Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory response. Science Advances. 2: e1501257. PMID 26989780 DOI: 10.1126/Sciadv.1501257 |
0.472 |
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| 2016 |
Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D, Knapp S, Knesl P, Kornigg S, Müller S, Nar H, et al. Structure-based design of an in vivo active selective BRD9 inhibitor. Journal of Medicinal Chemistry. PMID 26914985 DOI: 10.1021/Acs.Jmedchem.5B01865 |
0.347 |
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| 2016 |
Sorrell FJ, Szklarz M, Abdul Azeez KR, Elkins JM, Knapp S. Family-wide Structural Analysis of Human Numb-Associated Protein Kinases. Structure (London, England : 1993). PMID 26853940 DOI: 10.1016/j.str.2015.12.015 |
0.326 |
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| 2016 |
Raux B, Voitovich Y, Derviaux C, Lugari A, Rebuffet E, Milhas S, Priet S, Roux T, Trinquet E, Guillemot JC, Knapp S, Brunel JM, Fedorov AY, Collette Y, Roche P, et al. Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins. Journal of Medicinal Chemistry. PMID 26735842 DOI: 10.1021/acs.jmedchem.5b01708 |
0.356 |
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| 2016 |
Chaikuad A, Lang S, Brennan PE, Temperini C, Fedorov O, Hollander J, Nachane R, Abell C, Müller S, Siegal G, Knapp S. Structure-based identification of inhibitory fragments targeting the p300/CBP-associated factor bromodomain. Journal of Medicinal Chemistry. PMID 26731131 DOI: 10.1021/Acs.Jmedchem.5B01719 |
0.33 |
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| 2015 |
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie (Weinheim An Der Bergstrasse, Germany). 127: 6315-6319. PMID 27346896 DOI: 10.1002/ange.201501394 |
0.312 |
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| 2015 |
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Hing Che K, ... ... Knapp S, et al. Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy. Cancer Research. PMID 26552700 DOI: 10.1158/0008-5472.Can-15-0236 |
0.366 |
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| 2015 |
Knapp S. Emerging Target Families: Intractable Targets. Handbook of Experimental Pharmacology. PMID 26552403 DOI: 10.1007/164_2015_28 |
0.319 |
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| 2015 |
Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, ... ... Knapp S, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nature Biotechnology. PMID 26501955 DOI: 10.1038/Nbt.3374 |
0.382 |
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| 2015 |
Müller S, Chaikuad A, Gray NS, Knapp S. The ins and outs of selective kinase inhibitor development. Nature Chemical Biology. 11: 818-21. PMID 26485069 DOI: 10.1038/nchembio.1938 |
0.315 |
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| 2015 |
Gato-Cañas M, Martinez de Morentin X, Blanco-Luquin I, Fernandez-Irigoyen J, Zudaire I, Liechtenstein T, Arasanz H, Lozano T, Casares N, Chaikuad A, Knapp S, Guerrero-Setas D, Escors D, Kochan G, Santamaría E. A core of kinase-regulated interactomes defines the neoplastic MDSC lineage. Oncotarget. 6: 27160-75. PMID 26320174 DOI: 10.18632/oncotarget.4746 |
0.303 |
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| 2015 |
Alexander LT, Möbitz H, Drueckes P, Savitsky P, Fedorov O, Elkins JM, Deane CM, Cowan-Jacob SW, Knapp S. Type II Inhibitors Targeting CDK2. Acs Chemical Biology. PMID 26158339 DOI: 10.1021/acschembio.5b00398 |
0.359 |
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| 2015 |
Harrington L, Alexander LT, Knapp S, Bayley H. Pim Kinase Inhibitors Evaluated with a Single-Molecule Engineered Nanopore Sensor. Angewandte Chemie (International Ed. in English). PMID 26058458 DOI: 10.1002/Anie.201503141 |
0.301 |
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| 2015 |
Bennett J, Fedorov O, Tallant C, Monteiro O, Meier J, Gamble V, Savitsky P, Nunez-Alonso GA, Haendler B, Rogers C, Brennan PE, Müller S, Knapp S. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. Journal of Medicinal Chemistry. PMID 25974391 DOI: 10.1021/Acs.Jmedchem.5B00458 |
0.413 |
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| 2015 |
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie (International Ed. in English). 54: 6217-21. PMID 25864491 DOI: 10.1002/Anie.201501394 |
0.312 |
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| 2015 |
Martin E, Knapp S, Engh RA, Moebitz H, Varin T, Roux B, Meiler J, Berdini V, Baumann A, Vieth M. Perspective on computational and structural aspects of kinase discovery from IPK2014. Biochimica Et Biophysica Acta. PMID 25861861 DOI: 10.1016/J.Bbapap.2015.03.014 |
0.381 |
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| 2015 |
Kovackova S, Chang L, Bekerman E, Neveu G, Barouch-Bentov R, Chaikuad A, Heroven C, Šála M, De Jonghe S, Knapp S, Einav S, Herdewijn P. Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents. Journal of Medicinal Chemistry. 58: 3393-410. PMID 25822739 DOI: 10.1021/Jm501759M |
0.313 |
|
| 2015 |
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, ... ... Knapp S, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. Journal of Medicinal Chemistry. PMID 25799074 DOI: 10.1021/Acs.Jmedchem.5B00209 |
0.394 |
|
| 2015 |
Falke H, Chaikuad A, Becker A, Loaëc N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C. 10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A. Journal of Medicinal Chemistry. 58: 3131-43. PMID 25730262 DOI: 10.1021/jm501994d |
0.379 |
|
| 2015 |
Drouin L, McGrath S, Vidler LR, Chaikuad A, Monteiro O, Tallant C, Philpott M, Rogers C, Fedorov O, Liu M, Akhtar W, Hayes A, Raynaud F, Müller S, Knapp S, et al. Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. Journal of Medicinal Chemistry. 58: 2553-9. PMID 25719566 DOI: 10.1021/Jm501963E |
0.369 |
|
| 2015 |
Kestav K, Lavogina D, Raidaru G, Chaikuad A, Knapp S, Uri A. Bisubstrate inhibitor approach for targeting mitotic kinase Haspin. Bioconjugate Chemistry. 26: 225-34. PMID 25595038 DOI: 10.1021/bc500464r |
0.381 |
|
| 2015 |
Wilbek TS, Skovgaard T, Sorrell FJ, Knapp S, Berthelsen J, Strømgaard K. Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1. Chembiochem : a European Journal of Chemical Biology. 16: 59-63. PMID 25382253 DOI: 10.1002/cbic.201402512 |
0.325 |
|
| 2015 |
Homan KT, Larimore KM, Elkins JM, Szklarz M, Knapp S, Tesmer JJ. Identification and structure-function analysis of subfamily selective g protein-coupled receptor kinase inhibitors. Acs Chemical Biology. 10: 310-9. PMID 25238254 DOI: 10.1021/Cb5006323 |
0.396 |
|
| 2014 |
Wang J, Knapp S, Pyne NJ, Pyne S, Elkins JM. Crystal Structure of Sphingosine Kinase 1 with PF-543. Acs Medicinal Chemistry Letters. 5: 1329-33. PMID 25516793 DOI: 10.1021/ml5004074 |
0.31 |
|
| 2014 |
Chaikuad A, Tacconi EM, Zimmer J, Liang Y, Gray NS, Tarsounas M, Knapp S. A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics. Nature Chemical Biology. 10: 853-60. PMID 25195011 DOI: 10.1038/Nchembio.1629 |
0.335 |
|
| 2014 |
Knapp S, Sundström M. Recently targeted kinases and their inhibitors-the path to clinical trials. Current Opinion in Pharmacology. 17: 58-63. PMID 25113945 DOI: 10.1016/j.coph.2014.07.015 |
0.351 |
|
| 2014 |
Philpott M, Rogers CM, Yapp C, Wells C, Lambert JP, Strain-Damerell C, Burgess-Brown NA, Gingras AC, Knapp S, Müller S. Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching. Epigenetics & Chromatin. 7: 14. PMID 25097667 DOI: 10.1186/1756-8935-7-14 |
0.361 |
|
| 2014 |
Hay DA, Fedorov O, Martin S, Singleton DC, Tallant C, Wells C, Picaud S, Philpott M, Monteiro OP, Rogers CM, Conway SJ, Rooney TP, Tumber A, Yapp C, Filippakopoulos P, ... ... Knapp S, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. Journal of the American Chemical Society. 136: 9308-19. PMID 24946055 DOI: 10.1021/Ja412434F |
0.324 |
|
| 2014 |
Rudolf AF, Skovgaard T, Knapp S, Jensen LJ, Berthelsen J. A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination. Plos One. 9: e98800. PMID 24915177 DOI: 10.1371/journal.pone.0098800 |
0.345 |
|
| 2014 |
Filippakopoulos P, Knapp S. Targeting bromodomains: epigenetic readers of lysine acetylation. Nature Reviews. Drug Discovery. 13: 337-56. PMID 24751816 DOI: 10.1038/nrd4286 |
0.344 |
|
| 2014 |
Maiolica A, de Medina-Redondo M, Schoof EM, Chaikuad A, Villa F, Gatti M, Jeganathan S, Lou HJ, Novy K, Hauri S, Toprak UH, Herzog F, Meraldi P, Penengo L, Turk BE, ... Knapp S, et al. Modulation of the chromatin phosphoproteome by the Haspin protein kinase. Molecular & Cellular Proteomics : McP. 13: 1724-40. PMID 24732914 DOI: 10.1074/Mcp.M113.034819 |
0.33 |
|
| 2014 |
Zhao Z, Wu H, Wang L, Liu Y, Knapp S, Liu Q, Gray NS. Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery? Acs Chemical Biology. 9: 1230-41. PMID 24730530 DOI: 10.1021/Cb500129T |
0.343 |
|
| 2014 |
Huber KV, Salah E, Radic B, Gridling M, Elkins JM, Stukalov A, Jemth AS, Göktürk C, Sanjiv K, Strömberg K, Pham T, Berglund UW, Colinge J, Bennett KL, Loizou JI, ... ... Knapp S, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 508: 222-7. PMID 24695225 DOI: 10.1038/nature13194 |
0.362 |
|
| 2014 |
Cowan-Jacob SW, Jahnke W, Knapp S. Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases. Future Medicinal Chemistry. 6: 541-61. PMID 24649957 DOI: 10.4155/fmc.13.216 |
0.377 |
|
| 2014 |
Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nature Chemical Biology. 10: 305-12. PMID 24584101 DOI: 10.1038/Nchembio.1471 |
0.366 |
|
| 2014 |
Chaikuad A, Keates T, Vincke C, Kaufholz M, Zenn M, Zimmermann B, Gutiérrez C, Zhang RG, Hatzos-Skintges C, Joachimiak A, Muyldermans S, Herberg FW, Knapp S, Müller S. Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies. The Biochemical Journal. 459: 59-69. PMID 24438162 DOI: 10.1042/BJ20131399 |
0.37 |
|
| 2014 |
Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I, Marsden BD, Filippakopoulos P, Müller S, Knapp S, Brennan PE. [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. Journal of Medicinal Chemistry. 57: 462-76. PMID 24313754 DOI: 10.1021/Jm401568S |
0.336 |
|
| 2013 |
Ferguson FM, Fedorov O, Chaikuad A, Philpott M, Muniz JR, Felletar I, von Delft F, Heightman T, Knapp S, Abell C, Ciulli A. Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain. Journal of Medicinal Chemistry. 56: 10183-7. PMID 24304323 DOI: 10.1021/Jm401582C |
0.334 |
|
| 2013 |
Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proceedings of the National Academy of Sciences of the United States of America. 110: 19754-9. PMID 24248379 DOI: 10.1073/Pnas.1310658110 |
0.336 |
|
| 2013 |
Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. European Journal of Medicinal Chemistry. 70: 758-67. PMID 24239623 DOI: 10.1016/J.Ejmech.2013.10.052 |
0.321 |
|
| 2013 |
Vidler LR, Filippakopoulos P, Fedorov O, Picaud S, Martin S, Tomsett M, Woodward H, Brown N, Knapp S, Hoelder S. Discovery of novel small-molecule inhibitors of BRD4 using structure-based virtual screening. Journal of Medicinal Chemistry. 56: 8073-88. PMID 24090311 DOI: 10.1021/Jm4011302 |
0.308 |
|
| 2013 |
De Nicola GF, Martin ED, Chaikuad A, Bassi R, Clark J, Martino L, Verma S, Sicard P, Tata R, Atkinson RA, Knapp S, Conte MR, Marber MS. Mechanism and consequence of the autoactivation of p38α mitogen-activated protein kinase promoted by TAB1. Nature Structural & Molecular Biology. 20: 1182-90. PMID 24037507 DOI: 10.1038/nsmb.2668 |
0.303 |
|
| 2013 |
Lori C, Lantella A, Pasquo A, Alexander LT, Knapp S, Chiaraluce R, Consalvi V. Effect of single amino acid substitution observed in cancer on Pim-1 kinase thermodynamic stability and structure. Plos One. 8: e64824. PMID 23755147 DOI: 10.1371/journal.pone.0064824 |
0.314 |
|
| 2013 |
Soundararajan M, Roos AK, Savitsky P, Filippakopoulos P, Kettenbach AN, Olsen JV, Gerber SA, Eswaran J, Knapp S, Elkins JM. Structures of Down syndrome kinases, DYRKs, reveal mechanisms of kinase activation and substrate recognition. Structure (London, England : 1993). 21: 986-96. PMID 23665168 DOI: 10.1016/J.Str.2013.03.012 |
0.336 |
|
| 2013 |
Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. Journal of Medicinal Chemistry. 56: 4413-21. PMID 23656407 DOI: 10.1021/Jm4000837 |
0.4 |
|
| 2013 |
Lu M, Breyssens H, Salter V, Zhong S, Hu Y, Baer C, Ratnayaka I, Sullivan A, Brown NR, Endicott J, Knapp S, Kessler BM, Middleton MR, Siebold C, Jones EY, et al. Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP. Cancer Cell. 23: 618-33. PMID 23623661 DOI: 10.1016/j.ccr.2013.03.013 |
0.487 |
|
| 2013 |
Ekambaram R, Enkvist E, Vaasa A, Kasari M, Raidaru G, Knapp S, Uri A. Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1. Chemmedchem. 8: 909-13. PMID 23616352 DOI: 10.1002/cmdc.201300042 |
0.374 |
|
| 2013 |
Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Müller S, Schwaller J, ... ... Knapp S, et al. PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains. Cancer Research. 73: 3336-46. PMID 23576556 DOI: 10.1158/0008-5472.Can-12-3292 |
0.395 |
|
| 2013 |
Hewings DS, Fedorov O, Filippakopoulos P, Martin S, Picaud S, Tumber A, Wells C, Olcina MM, Freeman K, Gill A, Ritchie AJ, Sheppard DW, Russell AJ, Hammond EM, Knapp S, et al. Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands. Journal of Medicinal Chemistry. 56: 3217-27. PMID 23517011 DOI: 10.1021/Jm301588R |
0.324 |
|
| 2013 |
Yu W, Smil D, Li F, Tempel W, Fedorov O, Nguyen KT, Bolshan Y, Al-Awar R, Knapp S, Arrowsmith CH, Vedadi M, Brown PJ, Schapira M. Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorganic & Medicinal Chemistry. 21: 1787-94. PMID 23433670 DOI: 10.1016/J.Bmc.2013.01.049 |
0.361 |
|
| 2013 |
Cheng Z, Gong Y, Ma Y, Lu K, Lu X, Pierce LA, Thompson RC, Muller S, Knapp S, Wang J. Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 19: 1748-59. PMID 23403638 DOI: 10.1158/1078-0432.CCR-12-3066 |
0.331 |
|
| 2013 |
Myrianthopoulos V, Kritsanida M, Gaboriaud-Kolar N, Magiatis P, Ferandin Y, Durieu E, Lozach O, Cappel D, Soundararajan M, Filippakopoulos P, Sherman W, Knapp S, Meijer L, Mikros E, Skaltsounis AL. Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases. Acs Medicinal Chemistry Letters. 4: 22-26. PMID 23336033 DOI: 10.1021/ml300207a |
0.334 |
|
| 2013 |
Mehellou Y, Alessi DR, Macartney TJ, Szklarz M, Knapp S, Elkins JM. Structural insights into the activation of MST3 by MO25. Biochemical and Biophysical Research Communications. 431: 604-9. PMID 23296203 DOI: 10.1016/J.Bbrc.2012.12.113 |
0.334 |
|
| 2012 |
Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. Journal of Medicinal Chemistry. 55: 9831-7. PMID 23095041 DOI: 10.1021/Jm3010515 |
0.332 |
|
| 2012 |
Tahtouh T, Elkins JM, Filippakopoulos P, Soundararajan M, Burgy G, Durieu E, Cochet C, Schmid RS, Lo DC, Delhommel F, Oberholzer AE, Pearl LH, Carreaux F, Bazureau JP, Knapp S, et al. Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. Journal of Medicinal Chemistry. 55: 9312-30. PMID 22998443 DOI: 10.1021/jm301034u |
0.321 |
|
| 2012 |
Chaikuad A, Alfano I, Kerr G, Sanvitale CE, Boergermann JH, Triffitt JT, von Delft F, Knapp S, Knaus P, Bullock AN. Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva. The Journal of Biological Chemistry. 287: 36990-8. PMID 22977237 DOI: 10.1074/jbc.M112.365932 |
0.302 |
|
| 2012 |
Hewings DS, Rooney TP, Jennings LE, Hay DA, Schofield CJ, Brennan PE, Knapp S, Conway SJ. Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions. Journal of Medicinal Chemistry. 55: 9393-413. PMID 22924434 DOI: 10.1021/Jm300915B |
0.358 |
|
| 2012 |
Vidler LR, Brown N, Knapp S, Hoelder S. Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites. Journal of Medicinal Chemistry. 55: 7346-59. PMID 22788793 DOI: 10.1021/Jm300346W |
0.352 |
|
| 2012 |
Filippakopoulos P, Knapp S. The bromodomain interaction module. Febs Letters. 586: 2692-704. PMID 22710155 DOI: 10.1016/j.febslet.2012.04.045 |
0.304 |
|
| 2012 |
Hellwig S, Miduturu CV, Kanda S, Zhang J, Filippakopoulos P, Salah E, Deng X, Choi HG, Zhou W, Hur W, Knapp S, Gray NS, Smithgall TE. Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chemistry & Biology. 19: 529-40. PMID 22520759 DOI: 10.1016/J.Chembiol.2012.01.020 |
0.313 |
|
| 2012 |
Filippakopoulos P, Picaud S, Fedorov O, Keller M, Wrobel M, Morgenstern O, Bracher F, Knapp S. Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family. Bioorganic & Medicinal Chemistry. 20: 1878-86. PMID 22137933 DOI: 10.1016/j.bmc.2011.10.080 |
0.367 |
|
| 2012 |
Huber K, Brault L, Fedorov O, Gasser C, Filippakopoulos P, Bullock AN, Fabbro D, Trappe J, Schwaller J, Knapp S, Bracher F. 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes. Journal of Medicinal Chemistry. 55: 403-13. PMID 22136433 DOI: 10.1021/jm201286z |
0.37 |
|
| 2012 |
Fedorov O, Niesen FH, Knapp S. Kinase inhibitor selectivity profiling using differential scanning fluorimetry. Methods in Molecular Biology (Clifton, N.J.). 795: 109-18. PMID 21960218 DOI: 10.1007/978-1-61779-337-0_7 |
0.369 |
|
| 2011 |
Muller S, Filippakopoulos P, Knapp S. Bromodomains as therapeutic targets. Expert Reviews in Molecular Medicine. 13: e29. PMID 21933453 DOI: 10.1017/S1462399411001992 |
0.359 |
|
| 2011 |
Miduturu CV, Deng X, Kwiatkowski N, Yang W, Brault L, Filippakopoulos P, Chung E, Yang Q, Schwaller J, Knapp S, King RW, Lee JD, Herrgard S, Zarrinkar P, Gray NS. High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors. Chemistry & Biology. 18: 868-79. PMID 21802008 DOI: 10.1016/J.Chembiol.2011.05.010 |
0.347 |
|
| 2011 |
Debdab M, Carreaux F, Renault S, Soundararajan M, Fedorov O, Filippakopoulos P, Lozach O, Babault L, Tahtouh T, Baratte B, Ogawa Y, Hagiwara M, Eisenreich A, Rauch U, Knapp S, et al. Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. Journal of Medicinal Chemistry. 54: 4172-86. PMID 21615147 DOI: 10.1021/jm200274d |
0.315 |
|
| 2011 |
Feng L, Geisselbrecht Y, Blanck S, Wilbuer A, Atilla-Gokcumen GE, Filippakopoulos P, Kräling K, Celik MA, Harms K, Maksimoska J, Marmorstein R, Frenking G, Knapp S, Essen LO, Meggers E. Structurally sophisticated octahedral metal complexes as highly selective protein kinase inhibitors. Journal of the American Chemical Society. 133: 5976-86. PMID 21446733 DOI: 10.1021/Ja1112996 |
0.311 |
|
| 2011 |
Salah E, Ugochukwu E, Barr AJ, von Delft F, Knapp S, Elkins JM. Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. Journal of Medicinal Chemistry. 54: 2359-67. PMID 21417343 DOI: 10.1021/jm101506n |
0.361 |
|
| 2011 |
Fedorov O, Huber K, Eisenreich A, Filippakopoulos P, King O, Bullock AN, Szklarczyk D, Jensen LJ, Fabbro D, Trappe J, Rauch U, Bracher F, Knapp S. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chemistry & Biology. 18: 67-76. PMID 21276940 DOI: 10.1016/J.Chembiol.2010.11.009 |
0.408 |
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| 2010 |
Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, ... ... Knapp S, et al. Selective inhibition of BET bromodomains. Nature. 468: 1067-73. PMID 20871596 DOI: 10.1038/Nature09504 |
0.372 |
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| 2010 |
López-Ramos M, Prudent R, Moucadel V, Sautel CF, Barette C, Lafanechère L, Mouawad L, Grierson D, Schmidt F, Florent JC, Filippakopoulos P, Bullock AN, Knapp S, Reiser JB, Cochet C. New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 24: 3171-85. PMID 20400536 DOI: 10.1096/Fj.09-143743 |
0.391 |
|
| 2010 |
Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nature Chemical Biology. 6: 359-68. PMID 20383151 DOI: 10.1038/Nchembio.345 |
0.37 |
|
| 2010 |
Brault L, Gasser C, Bracher F, Huber K, Knapp S, Schwaller J. PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers. Haematologica. 95: 1004-15. PMID 20145274 DOI: 10.3324/haematol.2009.017079 |
0.365 |
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| 2010 |
Eswaran J, Knapp S. Insights into protein kinase regulation and inhibition by large scale structural comparison. Biochimica Et Biophysica Acta. 1804: 429-32. PMID 19854302 DOI: 10.1016/j.bbapap.2009.10.013 |
0.354 |
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| 2009 |
Eswaran J, Patnaik D, Filippakopoulos P, Wang F, Stein RL, Murray JW, Higgins JM, Knapp S. Structure and functional characterization of the atypical human kinase haspin. Proceedings of the National Academy of Sciences of the United States of America. 106: 20198-203. PMID 19918057 DOI: 10.1073/Pnas.0901989106 |
0.352 |
|
| 2009 |
Bullock AN, Russo S, Amos A, Pagano N, Bregman H, Debreczeni JE, Lee WH, von Delft F, Meggers E, Knapp S. Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor. Plos One. 4: e7112. PMID 19841674 DOI: 10.1371/Journal.Pone.0007112 |
0.331 |
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| 2009 |
Akué-Gédu R, Rossignol E, Azzaro S, Knapp S, Filippakopoulos P, Bullock AN, Bain J, Cohen P, Prudhomme M, Anizon F, Moreau P. Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors. Journal of Medicinal Chemistry. 52: 6369-81. PMID 19788246 DOI: 10.1021/Jm901018F |
0.375 |
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| 2009 |
Elkins JM, Amos A, Niesen FH, Pike AC, Fedorov O, Knapp S. Structure of dystrophia myotonica protein kinase. Protein Science : a Publication of the Protein Society. 18: 782-91. PMID 19309729 DOI: 10.1002/pro.82 |
0.31 |
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| 2009 |
Bullock AN, Das S, Debreczeni JE, Rellos P, Fedorov O, Niesen FH, Guo K, Papagrigoriou E, Amos AL, Cho S, Turk BE, Ghosh G, Knapp S. Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation. Structure (London, England : 1993). 17: 352-62. PMID 19278650 DOI: 10.1016/J.Str.2008.12.023 |
0.337 |
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| 2009 |
Barr AJ, Ugochukwu E, Lee WH, King ON, Filippakopoulos P, Alfano I, Savitsky P, Burgess-Brown NA, Müller S, Knapp S. Large-scale structural analysis of the classical human protein tyrosine phosphatome. Cell. 136: 352-63. PMID 19167335 DOI: 10.1016/j.cell.2008.11.038 |
0.351 |
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| 2009 |
Scheeff ED, Eswaran J, Bunkoczi G, Knapp S, Manning G. Structure of the pseudokinase VRK3 reveals a degraded catalytic site, a highly conserved kinase fold, and a putative regulatory binding site. Structure (London, England : 1993). 17: 128-38. PMID 19141289 DOI: 10.1016/J.Str.2008.10.018 |
0.316 |
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| 2008 |
Marsden BD, Knapp S. Doing more than just the structure-structural genomics in kinase drug discovery. Current Opinion in Chemical Biology. 12: 40-5. PMID 18267130 DOI: 10.1016/j.cbpa.2008.01.042 |
0.359 |
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| 2008 |
Eswaran J, Bernad A, Ligos JM, Guinea B, Debreczeni JE, Sobott F, Parker SA, Najmanovich R, Turk BE, Knapp S. Structure of the human protein kinase MPSK1 reveals an atypical activation loop architecture. Structure (London, England : 1993). 16: 115-24. PMID 18184589 DOI: 10.1016/J.Str.2007.10.026 |
0.301 |
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| 2007 |
Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proceedings of the National Academy of Sciences of the United States of America. 104: 20523-8. PMID 18077363 DOI: 10.1073/pnas.0708800104 |
0.391 |
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| 2007 |
Bunkoczi G, Salah E, Filippakopoulos P, Fedorov O, Müller S, Sobott F, Parker SA, Zhang H, Min W, Turk BE, Knapp S. Structural and functional characterization of the human protein kinase ASK1. Structure (London, England : 1993). 15: 1215-26. PMID 17937911 DOI: 10.1016/j.str.2007.08.011 |
0.358 |
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| 2007 |
Pogacic V, Bullock AN, Fedorov O, Filippakopoulos P, Gasser C, Biondi A, Meyer-Monard S, Knapp S, Schwaller J. Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. Cancer Research. 67: 6916-24. PMID 17638903 DOI: 10.1158/0008-5472.CAN-07-0320 |
0.369 |
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| 2007 |
Fedorov O, Sundström M, Marsden B, Knapp S. Insights for the development of specific kinase inhibitors by targeted structural genomics. Drug Discovery Today. 12: 365-72. PMID 17467572 DOI: 10.1016/j.drudis.2007.03.006 |
0.35 |
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| 2007 |
Eswaran J, Lee WH, Debreczeni JE, Filippakopoulos P, Turnbull A, Fedorov O, Deacon SW, Peterson JR, Knapp S. Crystal Structures of the p21-activated kinases PAK4, PAK5, and PAK6 reveal catalytic domain plasticity of active group II PAKs. Structure (London, England : 1993). 15: 201-13. PMID 17292838 DOI: 10.1016/j.str.2007.01.001 |
0.327 |
|
| 2007 |
Rellos P, Ivins FJ, Baxter JE, Pike A, Nott TJ, Parkinson DM, Das S, Howell S, Fedorov O, Shen QY, Fry AM, Knapp S, Smerdon SJ. Structure and regulation of the human Nek2 centrosomal kinase. The Journal of Biological Chemistry. 282: 6833-42. PMID 17197699 DOI: 10.1074/jbc.M609721200 |
0.358 |
|
| 2006 |
Barr AJ, Knapp S. MAPK-specific tyrosine phosphatases: new targets for drug discovery? Trends in Pharmacological Sciences. 27: 525-30. PMID 16919785 DOI: 10.1016/J.TIPS.2006.08.005 |
0.392 |
|
| 2006 |
Kavanagh KL, Guo K, Dunford JE, Wu X, Knapp S, Ebetino FH, Rogers MJ, Russell RG, Oppermann U. The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs. Proceedings of the National Academy of Sciences of the United States of America. 103: 7829-34. PMID 16684881 DOI: 10.1073/pnas.0601643103 |
0.326 |
|
| 2006 |
Eswaran J, von Kries JP, Marsden B, Longman E, Debreczeni JE, Ugochukwu E, Turnbull A, Lee WH, Knapp S, Barr AJ. Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases. The Biochemical Journal. 395: 483-91. PMID 16441242 DOI: 10.1042/BJ20051931 |
0.375 |
|
| 2005 |
Bullock AN, Debreczeni JE, Fedorov OY, Nelson A, Marsden BD, Knapp S. Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase. Journal of Medicinal Chemistry. 48: 7604-14. PMID 16302800 DOI: 10.1021/Jm0504858 |
0.403 |
|
| 2005 |
Bullock AN, Debreczeni J, Amos AL, Knapp S, Turk BE. Structure and substrate specificity of the Pim-1 kinase. The Journal of Biological Chemistry. 280: 41675-82. PMID 16227208 DOI: 10.1074/jbc.M510711200 |
0.326 |
|
| 2004 |
Faria TQ, Knapp S, Ladenstein R, Maçanita AL, Santos H. Protein stabilisation by compatible solutes: effect of mannosylglycerate on unfolding thermodynamics and activity of ribonuclease A. Chembiochem : a European Journal of Chemical Biology. 4: 734-41. PMID 12898624 DOI: 10.1002/Cbic.200300574 |
0.591 |
|
| 2003 |
Lolli G, Thaler F, Valsasina B, Roletto F, Knapp S, Uggeri M, Bachi A, Matafora V, Storici P, Stewart A, Kalisz HM, Isacchi A. Inhibitor affinity chromatography: Profiling the specific reactivity of the proteome with immobilized molecules Proteomics. 3: 1287-1298. PMID 12872229 DOI: 10.1002/pmic.200300431 |
0.392 |
|
| 2002 |
Filling C, Berndt KD, Benach J, Knapp S, Prozorovski T, Nordling E, Ladenstein R, Jörnvall H, Oppermann U. Critical residues for structure and catalysis in short-chain dehydrogenases/reductases. The Journal of Biological Chemistry. 277: 25677-84. PMID 11976334 DOI: 10.1074/jbc.M202160200 |
0.608 |
|
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