| Year |
Citation |
Score |
| 2023 |
Rahman SN, McNaught-Flores DA, Huppelschoten Y, da Costa Pereira D, Christopoulos A, Leurs R, Langmead CJ. Structural and Molecular Determinants for Isoform Bias at Human Histamine H Receptor Isoforms. Acs Chemical Neuroscience. PMID 36702158 DOI: 10.1021/acschemneuro.2c00425 |
0.345 |
|
| 2022 |
Saito A, Alvi S, Christopoulos A, Valant C, Carbone SE, Poole DP. Therapeutic potential of allosteric modulators for the treatment of gastrointestinal motility disorders. British Journal of Pharmacology. PMID 36565295 DOI: 10.1111/bph.16023 |
0.482 |
|
| 2022 |
Jiang Y, Yeasmin M, Gondin AB, Christopoulos A, Valant C, Burger WAC, Thal DM. Importance of receptor expression in the classification of novel ligands at the M muscarinic acetylcholine receptor. British Journal of Pharmacology. PMID 36550621 DOI: 10.1111/bph.16021 |
0.482 |
|
| 2022 |
Piper SJ, Deganutti G, Lu J, Zhao P, Liang YL, Lu Y, Fletcher MM, Hossain MA, Christopoulos A, Reynolds CA, Danev R, Sexton PM, Wootten D. Understanding VPAC receptor family peptide binding and selectivity. Nature Communications. 13: 7013. PMID 36385145 DOI: 10.1038/s41467-022-34629-3 |
0.355 |
|
| 2022 |
Dwomoh L, Rossi M, Scarpa M, Khajehali E, Molloy C, Herzyk P, Mistry SN, Bottrill AR, Sexton PM, Christopoulos A, Conn J, Lindsley CW, Bradley SJ, Tobin AB. M muscarinic receptor activation reduces the molecular pathology and slows the progression of prion-mediated neurodegenerative disease. Science Signaling. 15: eabm3720. PMID 36378750 DOI: 10.1126/scisignal.abm3720 |
0.436 |
|
| 2022 |
Nguyen HTM, van der Westhuizen ET, Langmead CJ, Tobin AB, Sexton PM, Christopoulos A, Valant C. Opportunities and challenges for the development of M1 muscarinic receptor positive allosteric modulators in the treatment for neurocognitive deficits. British Journal of Pharmacology. PMID 36355830 DOI: 10.1111/bph.15982 |
0.766 |
|
| 2022 |
Deo O, Alvi S, Pham V, Christopoulos A, Thal DM, Jörg M, Capuano B, Valant C, Scammells PJ. The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δOpioid Receptor. Journal of Medicinal Chemistry. 65: 12367-12385. PMID 36099150 DOI: 10.1021/acs.jmedchem.2c01061 |
0.339 |
|
| 2022 |
Awalt JK, Nguyen ATN, Fyfe TJ, Thai BS, White PJ, Christopoulos A, Jörg M, May LT, Scammells PJ. Examining the Role of the Linker in Bitopic -Substituted Adenosine Derivatives Acting as Biased Adenosine A Receptor Agonists. Journal of Medicinal Chemistry. PMID 35729775 DOI: 10.1021/acs.jmedchem.2c00320 |
0.382 |
|
| 2022 |
McDonald JK, van der Westhuizen ET, Pham V, Thompson G, Felder CC, Paul SM, Thal DM, Christopoulos A, Valant C. Biased Profile of Xanomeline at the Recombinant Human M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 35380782 DOI: 10.1021/acschemneuro.1c00827 |
0.781 |
|
| 2022 |
Wakeham MCL, Davie BJ, Chalmers DK, Christopoulos A, Capuano B, Valant C, Scammells PJ. Structural Features of Iperoxo-BQCA Muscarinic Acetylcholine Receptor Hybrid Ligands Determining Subtype Selectivity and Efficacy. Acs Chemical Neuroscience. 13: 97-111. PMID 34905693 DOI: 10.1021/acschemneuro.1c00572 |
0.528 |
|
| 2021 |
Brown AJH, Bradley SJ, Marshall FH, Brown GA, Bennett KA, Brown J, Cansfield JE, Cross DM, de Graaf C, Hudson BD, Dwomoh L, Dias JM, Errey JC, Hurrell E, Liptrot J, ... ... Christopoulos A, et al. From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease. Cell. 184: 5886-5901.e22. PMID 34822784 DOI: 10.1016/j.cell.2021.11.001 |
0.45 |
|
| 2021 |
DiCello JJ, Carbone SE, Saito A, Pham V, Szymaszkiewicz A, Gondin AB, Alvi S, Marique K, Shenoy P, Veldhuis NA, Fichna J, Canals M, Christopoulos A, Valant C, Poole DP. Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gut motility disorders. American Journal of Physiology. Gastrointestinal and Liver Physiology. PMID 34755545 DOI: 10.1152/ajpgi.00297.2021 |
0.381 |
|
| 2021 |
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Southan C, Davies JA, Abbracchio MP, Alexander W, et al. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors. British Journal of Pharmacology. 178: S27-S156. PMID 34529832 DOI: 10.1111/bph.15538 |
0.384 |
|
| 2021 |
Alexander SP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Southan C, Buneman OP, Cidlowski JA, Christopoulos A, Davenport AP, Fabbro D, et al. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Introduction and Other Protein Targets. British Journal of Pharmacology. 178: S1-S26. PMID 34529830 DOI: 10.1111/bph.15537 |
0.362 |
|
| 2021 |
Draper-Joyce CJ, Bhola R, Wang J, Bhattarai A, Nguyen ATN, Cowie-Kent I, O'Sullivan K, Chia LY, Venugopal H, Valant C, Thal DM, Wootten D, Panel N, Carlsson J, Christie MJ, ... ... Christopoulos A, et al. Positive allosteric mechanisms of adenosine A receptor-mediated analgesia. Nature. PMID 34497422 DOI: 10.1038/s41586-021-03897-2 |
0.369 |
|
| 2021 |
Burger WAC, Gentry PR, Berizzi AE, Vuckovic Z, van der Westhuizen ET, Thompson G, Yeasmin M, Lindsley CW, Sexton PM, Langmead CJ, Tobin AB, Christopoulos A, Valant C, Thal DM. Identification of a Novel Allosteric Site at the M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 34351123 DOI: 10.1021/acschemneuro.1c00383 |
0.768 |
|
| 2021 |
Josephs TM, Belousoff MJ, Liang YL, Piper SJ, Cao J, Garama DJ, Leach K, Gregory KJ, Christopoulos A, Hay DL, Danev R, Wootten D, Sexton PM. Structure and dynamics of the CGRP receptor in apo and peptide-bound forms. Science (New York, N.Y.). PMID 33602864 DOI: 10.1126/science.abf7258 |
0.327 |
|
| 2020 |
van der Westhuizen ET, Choy KHC, Valant C, McKenzie-Nickson S, Bradley SJ, Tobin AB, Sexton PM, Christopoulos A. Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias. Frontiers in Pharmacology. 11: 606656. PMID 33584282 DOI: 10.3389/fphar.2020.606656 |
0.806 |
|
| 2020 |
Khajehali E, Bradley S, van der Westhuizen ET, Molloy C, Valant C, Finlayson L, Lindsley CW, Sexton PM, Tobin AB, Christopoulos A. Restoring Agonist Function at a Chemogenetically Modified M Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 33196174 DOI: 10.1021/acschemneuro.0c00540 |
0.793 |
|
| 2020 |
Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD, Liang YL, Glukhova A, Venugopal H, Christopoulos A, Furness SGB, et al. Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists. Molecular Cell. PMID 33027691 DOI: 10.1016/j.molcel.2020.09.020 |
0.34 |
|
| 2020 |
Scammells PJ, Jörg M, Khajehali E, van der Westhuizen ET, Choy KHC, Shackleford D, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A. Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. Chemmedchem. PMID 32851779 DOI: 10.1002/cmdc.202000540 |
0.78 |
|
| 2020 |
Hellyer SD, Sengmany K, Keller AN, Christopoulos A, Leach K, Gregory KJ. Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site. Biochemical Pharmacology. 114013. PMID 32389635 DOI: 10.1016/j.bcp.2020.114013 |
0.475 |
|
| 2020 |
Sengmany K, Hellyer SD, Christopoulos A, Lapinsky DJ, Leach K, Gregory KJ. Differential contribution of metabotropic glutamate receptor 5 common allosteric binding site residues to biased allosteric agonism. Biochemical Pharmacology. 114011. PMID 32380090 DOI: 10.1016/j.bcp.2020.114011 |
0.365 |
|
| 2020 |
Liang YL, Belousoff MJ, Fletcher MM, Zhang X, Khoshouei M, Deganutti G, Koole C, Furness SGB, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Danev R, Wootten D, Sexton PM. Structure and Dynamics of Adrenomedullin Receptors AM and AM Reveal Key Mechanisms in the Control of Receptor Phenotype by Receptor Activity-Modifying Proteins. Acs Pharmacology & Translational Science. 3: 263-284. PMID 32296767 DOI: 10.1021/acsptsci.9b00080 |
0.401 |
|
| 2020 |
Dong M, Harikumar KG, Raval SR, Milburn JE, Clark C, Alcala-Torano R, Mobarec JC, Reynolds CA, Ghirlanda G, Christopoulos A, Wootten D, Sexton PM, Miller LJ. Rational development of a high-affinity secretin receptor antagonist. Biochemical Pharmacology. 113929. PMID 32217097 DOI: 10.1016/J.Bcp.2020.113929 |
0.391 |
|
| 2020 |
Bradley SJ, Molloy C, Valuskova P, Dwomoh L, Scarpa M, Rossi M, Finlayson L, Svensson KA, Chernet E, Barth VN, Gherbi K, Sykes DA, Wilson CA, Mistry R, Sexton PM, ... Christopoulos A, et al. Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs. Nature Chemical Biology. 16: 240-249. PMID 32080630 DOI: 10.1038/S41589-019-0453-9 |
0.532 |
|
| 2020 |
Liang YL, Belousoff MJ, Zhao P, Koole C, Fletcher MM, Truong TT, Julita V, Christopoulos G, Xu HE, Zhang Y, Khoshouei M, Christopoulos A, Danev R, Sexton PM, Wootten D. Toward a Structural Understanding of Class B GPCR Peptide Binding and Activation. Molecular Cell. PMID 32004469 DOI: 10.1016/J.Molcel.2020.01.012 |
0.375 |
|
| 2020 |
Zhao P, Liang YL, Belousoff MJ, Deganutti G, Fletcher MM, Willard FS, Bell MG, Christe ME, Sloop KW, Inoue A, Truong TT, Clydesdale L, Furness SGB, Christopoulos A, Wang MW, et al. Activation of the GLP-1 receptor by a non-peptidic agonist. Nature. PMID 31915381 DOI: 10.1038/S41586-019-1902-Z |
0.378 |
|
| 2019 |
Pham V, Zhu Y, Dal Maso E, Reynolds CA, Deganutti G, Atanasio S, Hick CA, Yang D, Christopoulos A, Hay DL, Furness SGB, Wang MW, Wootten D, Sexton PM. Deconvoluting the Molecular Control of Binding and Signaling at the Amylin 3 Receptor: RAMP3 Alters Signal Propagation through Extracellular Loops of the Calcitonin Receptor. Acs Pharmacology & Translational Science. 2: 183-197. PMID 32219220 DOI: 10.1021/acsptsci.9b00010 |
0.338 |
|
| 2019 |
Dal Maso E, Glukhova A, Zhu Y, Garcia-Nafria J, Tate CG, Atanasio S, Reynolds CA, Ramírez-Aportela E, Carazo JM, Hick CA, Furness SGB, Hay DL, Liang YL, Miller LJ, Christopoulos A, et al. The Molecular Control of Calcitonin Receptor Signaling. Acs Pharmacology & Translational Science. 2: 31-51. PMID 32219215 DOI: 10.1021/acsptsci.8b00056 |
0.326 |
|
| 2019 |
Vuckovic Z, Gentry PR, Berizzi AE, Hirata K, Varghese S, Thompson G, van der Westhuizen ET, Burger WAC, Rahmani R, Valant C, Langmead CJ, Lindsley CW, Baell JB, Tobin AB, Sexton PM, ... Christopoulos A, et al. Crystal structure of the M muscarinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America. PMID 31772027 DOI: 10.2210/Pdb6Ol9/Pdb |
0.767 |
|
| 2019 |
Alexander SP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Buneman OP, Cidlowski JA, Christopoulos A, Davenport AP, et al. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Introduction and Other Protein Targets. British Journal of Pharmacology. 176: S1-S20. PMID 31710719 DOI: 10.1111/Bph.14747 |
0.38 |
|
| 2019 |
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Mathie A, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors. British Journal of Pharmacology. 176: S21-S141. PMID 31710717 DOI: 10.1111/Bph.14748 |
0.398 |
|
| 2019 |
Klein Herenbrink C, Verma R, Lim HD, Kopinathan A, Keen A, Shonberg J, Draper-Joyce CJ, Scammells PJ, Christopoulos A, Javitch JA, Capuano B, Shi L, Lane JR. Molecular determinants of the intrinsic efficacy of the antipsychotic aripiprazole. Acs Chemical Biology. PMID 31339684 DOI: 10.1021/Acschembio.9B00342 |
0.395 |
|
| 2019 |
Hollingsworth SA, Kelly B, Valant C, Michaelis JA, Mastromihalis O, Thompson G, Venkatakrishnan AJ, Hertig S, Scammells PJ, Sexton PM, Felder CC, Christopoulos A, Dror RO. Cryptic pocket formation underlies allosteric modulator selectivity at muscarinic GPCRs. Nature Communications. 10: 3289. PMID 31337749 DOI: 10.1038/s41467-019-11062-7 |
0.58 |
|
| 2018 |
Gregory KJ, Kufareva I, Keller AN, Khajehali E, Mun HC, Goolam MA, Mason RS, Capuano B, Conigrave AD, Christopoulos A, Leach K. Dual Action Calcium-Sensing Receptor Modulator Unmasks Novel Mode-Switching Mechanism. Acs Pharmacology & Translational Science. 1: 96-109. PMID 32219206 DOI: 10.1021/acsptsci.8b00021 |
0.404 |
|
| 2018 |
Glukhova A, Draper-Joyce CJ, Sunahara RK, Christopoulos A, Wootten D, Sexton PM. Rules of Engagement: GPCRs and G Proteins. Acs Pharmacology & Translational Science. 1: 73-83. PMID 32219204 DOI: 10.1021/acsptsci.8b00026 |
0.364 |
|
| 2018 |
Thompson KJ, Khajehali E, Bradley SJ, Navarrete JS, Huang XP, Slocum S, Jin J, Liu J, Xiong Y, Olsen RHJ, Diberto JF, Boyt KM, Pina MM, Pati D, Molloy C, ... ... Christopoulos A, et al. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs and . Acs Pharmacology & Translational Science. 1: 61-72. PMID 30868140 DOI: 10.1021/acsptsci.8b00012 |
0.376 |
|
| 2018 |
Desai AJ, Mechin I, Nagarajan K, Valant C, Wootten D, Lam PCH, Orry A, Abagyan R, Nair A, Sexton PM, Christopoulos A, Miller LJ. Molecular basis of action of a small molecule positive allosteric modulator (PAM)-agonist at the type 1 cholecystokinin holoreceptor. Molecular Pharmacology. PMID 30591538 DOI: 10.1124/Mol.118.114082 |
0.458 |
|
| 2018 |
Jörg M, van der Westhuizen ET, Khajehali E, Burger WAC, White JM, Choy KHC, Tobin AB, Sexton PM, Valant C, Capuano B, Christopoulos A, Scammells PJ. 6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity. Acs Chemical Neuroscience. PMID 30547573 DOI: 10.1021/acschemneuro.8b00613 |
0.792 |
|
| 2018 |
Miao Y, Bhattarai A, Nguyen ATN, Christopoulos A, May LT. Structural Basis for Binding of Allosteric Drug Leads in the Adenosine A Receptor. Scientific Reports. 8: 16836. PMID 30442899 DOI: 10.1038/S41598-018-35266-X |
0.398 |
|
| 2018 |
Riddy DM, Cook AE, Shackleford DM, Pierce TL, Mocaer E, Mannoury la Cour C, Sors A, Charman WN, Summers RJ, Sexton PM, Christopoulos A, Langmead CJ. Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H receptor antagonists. Neuropharmacology. PMID 30359639 DOI: 10.1016/j.neuropharm.2018.10.028 |
0.444 |
|
| 2018 |
Liang YL, Khoshouei M, Deganutti G, Glukhova A, Koole C, Peat TS, Radjainia M, Plitzko JM, Baumeister W, Miller LJ, Hay DL, Christopoulos A, Reynolds CA, Wootten D, Sexton PM. Cryo-EM structure of the active, G-protein complexed, human CGRP receptor. Nature. PMID 30209400 DOI: 10.1038/S41586-018-0535-Y |
0.364 |
|
| 2018 |
Fletcher MM, Halls ML, Zhao P, Clydesdale L, Christopoulos A, Sexton PM, Wootten D. Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists. Biochemical Pharmacology. PMID 30195733 DOI: 10.1016/j.bcp.2018.09.003 |
0.38 |
|
| 2018 |
Wootten D, Christopoulos A, Marti-Solano M, Babu MM, Sexton PM. Mechanisms of signalling and biased agonism in G protein-coupled receptors. Nature Reviews. Molecular Cell Biology. PMID 30104700 DOI: 10.1038/s41580-018-0049-3 |
0.444 |
|
| 2018 |
Draper-Joyce CJ, Khoshouei M, Thal DM, Liang YL, Nguyen ATN, Furness SGB, Venugopal H, Baltos JA, Plitzko JM, Danev R, Baumeister W, May LT, Wootten D, Sexton PM, Glukhova A, ... Christopoulos A, et al. Structure of the adenosine-bound human adenosine A receptor-G complex. Nature. PMID 29925945 DOI: 10.1038/S41586-018-0236-6 |
0.313 |
|
| 2018 |
Khajehali E, Valant C, Jörg M, Tobin AB, Jeffrey Conn P, Lindsley CW, Sexton PM, Scammells PJ, Christopoulos A. Probing the binding site of novel selective positive allosteric modulators at the M mAChR. Biochemical Pharmacology. PMID 29777683 DOI: 10.1016/J.Bcp.2018.05.009 |
0.497 |
|
| 2018 |
Lei S, Clydesdale L, Dai A, Cai X, Feng Y, Yang D, Liang YL, Koole C, Zhao P, Coudrat T, Christopoulos A, Wang MW, Wootten D, Sexton PM. Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism. The Journal of Biological Chemistry. PMID 29717000 DOI: 10.1074/jbc.RA118.003278 |
0.383 |
|
| 2018 |
Diepenhorst NA, Leach K, Keller AN, Rueda P, Cook AE, Pierce TL, Nowell C, Pastoureau P, Sabatini M, Summers RJ, Charman WN, Sexton PM, Christopoulos A, Langmead CJ. Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity. British Journal of Pharmacology. PMID 29714810 DOI: 10.1111/Bph.14344 |
0.301 |
|
| 2018 |
Bradley SJ, Molloy C, Bundgaard C, Mogg AJ, Thompson KJ, Dwomoh L, Sanger HE, Crabtree M, Brooke SM, Sexton PM, Felder CC, Christopoulos A, Broad LM, Tobin AB, Langmead CJ. Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes. Molecular Pharmacology. PMID 29695609 DOI: 10.1124/Mol.118.111872 |
0.56 |
|
| 2018 |
van der Westhuizen ET, Spathis A, Khajehali E, Jörg M, Mistry SN, Capuano B, Tobin AB, Sexton PM, Scammells PJ, Valant C, Christopoulos A. Assessment of the Molecular Mechanisms of Action of Novel 4-Phenylpyridine-2-One and 6-Phenylpyrimidin-4-One Allosteric Modulators at the M Muscarinic Acetylcholine Receptors. Molecular Pharmacology. 94: 770-783. PMID 29691279 DOI: 10.1124/mol.118.111633 |
0.789 |
|
| 2018 |
Berizzi A, Bender AM, Lindsley CW, Conn PJ, Sexton PM, Langmead C, Christopoulos A. Structure-activity relationships of pan-Gα coupled muscarinic acetylcholine receptor positive allosteric modulators. Acs Chemical Neuroscience. PMID 29683647 DOI: 10.1021/Acschemneuro.8B00136 |
0.599 |
|
| 2018 |
Vecchio EA, Baltos JA, Nguyen ATN, Christopoulos A, White PJ, May LT. New Paradigms in Adenosine Receptor Pharmacology: Allostery, Oligomerization and Biased Agonism. British Journal of Pharmacology. PMID 29679502 DOI: 10.1111/bph.14337 |
0.432 |
|
| 2018 |
Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead C, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neil JC, et al. Discovery and Optimization of Potent and CNS Penetrant M5-Preferring PAMs Derived From a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold. Acs Chemical Neuroscience. PMID 29678111 DOI: 10.1021/Acschemneuro.8B00126 |
0.43 |
|
| 2018 |
Keller AN, Kufareva I, Josephs TM, Diao J, Mai VT, Conigrave AD, Christopoulos A, Gregory KJ, Leach K. Identification of global and ligand-specific calcium sensing receptor activation mechanisms. Molecular Pharmacology. PMID 29636377 DOI: 10.1124/mol.118.112086 |
0.395 |
|
| 2018 |
Thal DM, Vuckovic Z, Draper-Joyce CJ, Liang YL, Glukhova A, Christopoulos A, Sexton PM. Recent advances in the determination of G protein-coupled receptor structures. Current Opinion in Structural Biology. 51: 28-34. PMID 29547818 DOI: 10.1016/j.sbi.2018.03.002 |
0.335 |
|
| 2018 |
Dallagnol JCC, Khajehali E, van der Westhuizen ET, Jörg M, Valant C, Gonçalves AG, Capuano B, Christopoulos A, Scammells PJ. Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the M Muscarinic Acetylcholine Receptor with Weak Agonist Activity and Diverse Modulatory Profiles. Journal of Medicinal Chemistry. 61: 2875-2894. PMID 29544056 DOI: 10.1021/acs.jmedchem.7b01812 |
0.784 |
|
| 2018 |
Liang YL, Khoshouei M, Glukhova A, Furness SGB, Zhao P, Clydesdale L, Koole C, Truong TT, Thal DM, Lei S, Radjainia M, Danev R, Baumeister W, Wang MW, Miller LJ, ... Christopoulos A, et al. Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor-Gs complex. Nature. PMID 29466332 DOI: 10.1038/Nature25773 |
0.323 |
|
| 2018 |
Dal Maso E, Zhu Y, Pham V, Reynolds CA, Deganutti G, Hick CA, Yang D, Christopoulos A, Hay DL, Wang MW, Sexton PM, Furness SGB, Wootten D. Extracellular loops 2 and 3 of the calcitonin receptor selectively modify agonist binding and efficacy. Biochemical Pharmacology. PMID 29454620 DOI: 10.1016/J.Bcp.2018.02.005 |
0.376 |
|
| 2018 |
Korczynska M, Clark MJ, Valant C, Xu J, Moo EV, Albold S, Weiss DR, Torosyan H, Huang W, Kruse AC, Lyda BR, May LT, Baltos JA, Sexton PM, Kobilka BK, ... Christopoulos A, et al. Structure-based discovery of selective positive allosteric modulators of antagonists for the Mmuscarinic acetylcholine receptor. Proceedings of the National Academy of Sciences of the United States of America. PMID 29453275 DOI: 10.1073/Pnas.1718037115 |
0.473 |
|
| 2018 |
Aurelio L, Baltos JA, Ford L, Nguyen ATN, Jörg M, Devine SM, Valant C, White PJ, Christopoulos A, May LT, Scammells PJ. A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists. Journal of Medicinal Chemistry. PMID 29446948 DOI: 10.1021/acs.jmedchem.8b00047 |
0.314 |
|
| 2018 |
Draper-Joyce CJ, Verma RK, Michino M, Shonberg J, Kopinathan A, Klein Herenbrink C, Scammells PJ, Capuano B, Abramyan AM, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions. Scientific Reports. 8: 1208. PMID 29352161 DOI: 10.1038/S41598-018-19642-1 |
0.357 |
|
| 2018 |
Draper-Joyce CJ, Michino M, Verma RK, Herenbrink CK, Shonberg J, Kopinathan A, Scammells PJ, Capuano B, Thal DM, Javitch JA, Christopoulos A, Shi L, Lane JR. The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor. Biochemical Pharmacology. PMID 29325769 DOI: 10.1016/J.Bcp.2018.01.002 |
0.384 |
|
| 2017 |
Coudrat T, Simms J, Christopoulos A, Wootten D, Sexton PM. Improving virtual screening of G protein-coupled receptors via ligand-directed modeling. Plos Computational Biology. 13: e1005819. PMID 29131821 DOI: 10.1371/journal.pcbi.1005819 |
0.361 |
|
| 2017 |
Fish I, Stoessel A, Eitel K, Valant C, Albold S, Hübner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P. Structure-based design and discovery of new M2 receptor agonists. Journal of Medicinal Chemistry. PMID 29094937 DOI: 10.1021/Acs.Jmedchem.7B01113 |
0.463 |
|
| 2017 |
Alexander SP, Christopoulos A, Davenport AP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA. THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: G protein-coupled receptors. British Journal of Pharmacology. 174: S17-S129. PMID 29055040 DOI: 10.1111/bph.13878 |
0.362 |
|
| 2017 |
Alexander SP, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Buneman OP, Cidlowski JA, Christopoulos A, Davenport AP, Fabbro D, Spedding M, et al. THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview. British Journal of Pharmacology. 174: S1-S16. PMID 29055037 DOI: 10.1111/Bph.13882 |
0.343 |
|
| 2017 |
Changeux JP, Christopoulos A. Allosteric modulation as a unifying mechanism for receptor function and regulation. Diabetes, Obesity & Metabolism. 19: 4-21. PMID 28880476 DOI: 10.1111/dom.12959 |
0.468 |
|
| 2017 |
Liang YL, Khoshouei M, Radjainia M, Zhang Y, Glukhova A, Tarrasch J, Thal DM, Furness SGB, Christopoulos G, Coudrat T, Danev R, Baumeister W, Miller LJ, Christopoulos A, Kobilka BK, et al. Phase-plate cryo-EM structure of a class B GPCR-G-protein complex. Nature. PMID 28437792 DOI: 10.1038/Nature22327 |
0.342 |
|
| 2017 |
Baltos JA, Vecchio EA, Harris MA, Qin CX, Ritchie RH, Christopoulos A, White PJ, May LT. Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism. Biochemical Pharmacology. PMID 28344125 DOI: 10.1016/j.bcp.2017.03.014 |
0.38 |
|
| 2017 |
Glukhova A, Thal DM, Nguyen AT, Vecchio EA, Jörg M, Scammells PJ, May LT, Sexton PM, Christopoulos A. Structure of the Adenosine A1 Receptor Reveals the Basis for Subtype Selectivity. Cell. 168: 867-877.e13. PMID 28235198 DOI: 10.1016/j.cell.2017.01.042 |
0.354 |
|
| 2016 |
Bradley SJ, Bourgognon JM, Sanger HE, Verity N, Mogg AJ, White DJ, Butcher AJ, Moreno JA, Molloy C, Macedo-Hatch T, Edwards JM, Wess J, Pawlak R, Read DJ, Sexton PM, ... ... Christopoulos A, et al. M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss. The Journal of Clinical Investigation. PMID 27991860 DOI: 10.1172/Jci87526 |
0.42 |
|
| 2016 |
Jörg M, Glukhova A, Abdul-Ridha A, Vecchio EA, Nguyen AT, Sexton PM, White PJ, May LT, Christopoulos A, Scammells PJ. Novel Irreversible Agonists Acting at the A1 Adenosine Receptor. Journal of Medicinal Chemistry. PMID 27958734 DOI: 10.1021/acs.jmedchem.6b01561 |
0.369 |
|
| 2016 |
Riddy DM, Cook A, Diepenhorst NA, Bosnyak S, Brady R, Mannoury-la-Cour C, Mocaer E, Summers RJ, Charman W, Sexton PM, Christopoulos A, Langmead CJ. Isoform-specific biased agonism of histamine H3 receptor agonists. Molecular Pharmacology. PMID 27864425 DOI: 10.1124/mol.116.106153 |
0.431 |
|
| 2016 |
Furness SG, Liang YL, Nowell CJ, Halls ML, Wookey PJ, Dal Maso E, Inoue A, Christopoulos A, Wootten D, Sexton PM. Ligand-Dependent Modulation of G Protein Conformation Alters Drug Efficacy. Cell. PMID 27720449 DOI: 10.1016/J.Cell.2016.09.021 |
0.354 |
|
| 2016 |
Nguyen AT, Baltos JA, Thomas T, Nguyen TD, Lopez Munoz L, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT. Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist efficacy. Molecular Pharmacology. PMID 27683014 DOI: 10.1124/mol.116.105007 |
0.455 |
|
| 2016 |
Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A. The role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling and cooperativity. Molecular Pharmacology. PMID 27683013 DOI: 10.1124/mol.116.105015 |
0.324 |
|
| 2016 |
Choy KH, Shackleford DM, Malone DT, Mistry SN, Patil RT, Scammells PJ, Langmead CJ, Pantelis C, Sexton PM, Lane JR, Christopoulos A. Positive allosteric modulation of the muscarinic M1 receptor improves efficacy of antipsychotics in mouse glutamatergic deficit models of behavior. The Journal of Pharmacology and Experimental Therapeutics. PMID 27630144 DOI: 10.1124/Jpet.116.235788 |
0.406 |
|
| 2016 |
Miao Y, Goldfeld DA, Moo EV, Sexton PM, Christopoulos A, McCammon JA, Valant C. Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor. Proceedings of the National Academy of Sciences of the United States of America. 113: E5675-84. PMID 27601651 DOI: 10.1073/Pnas.1612353113 |
0.57 |
|
| 2016 |
Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Furness SG, Miller LJ, Christopoulos A, Sexton PM. Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor. Biochemical Pharmacology. PMID 27569426 DOI: 10.1016/J.Bcp.2016.08.015 |
0.348 |
|
| 2016 |
Changeux JP, Christopoulos A. Allosteric Modulation as a Unifying Mechanism for Receptor Function and Regulation. Cell. 166: 1084-102. PMID 27565340 DOI: 10.1016/j.cell.2016.08.015 |
0.468 |
|
| 2016 |
Vecchio EA, Chuo CH, Baltos JA, Ford L, Scammells PJ, Wang BH, Christopoulos A, White PJ, May LT. The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. Biochemical Pharmacology. PMID 27520486 DOI: 10.1016/j.bcp.2016.08.007 |
0.368 |
|
| 2016 |
Berizzi A, Gentry PR, Rueda P, den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A. Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators. Molecular Pharmacology. PMID 27461343 DOI: 10.1124/mol.116.104182 |
0.556 |
|
| 2016 |
Sengmany K, Singh J, Stewart GD, Conn PJ, Christopoulos A, Gregory KJ. Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology. PMID 27392634 DOI: 10.1016/j.neuropharm.2016.07.001 |
0.479 |
|
| 2016 |
Wootten D, Reynolds CA, Smith KJ, Mobarec JC, Koole C, Savage EE, Pabreja K, Simms J, Sridhar R, Furness SG, Liu M, Thompson PE, Miller LJ, Christopoulos A, Sexton PM. The Extracellular Surface of the GLP-1 Receptor Is a Molecular Trigger for Biased Agonism. Cell. 165: 1632-1643. PMID 27315480 DOI: 10.1016/J.Cell.2016.05.023 |
0.433 |
|
| 2016 |
Thompson GL, Robert Lane J, Coudrat T, Sexton PM, Christopoulos A, Canals M. Systematic analysis of factors influencing observations of biased agonism at the mu-opioid receptor. Biochemical Pharmacology. PMID 27286929 DOI: 10.1016/j.bcp.2016.05.014 |
0.422 |
|
| 2016 |
Baltos JA, Paoletta S, Nguyen AT, Gregory KJ, Tosh DK, Christopoulos A, Jacobson KA, May LT. Structure-Activity Analysis of Biased Agonism at the Human Adenosine A3 Receptor. Molecular Pharmacology. PMID 27136943 DOI: 10.1124/Mol.116.103283 |
0.31 |
|
| 2016 |
Gregory KJ, Velagaleti R, Thal D, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ. Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. Acs Chemical Biology. PMID 27115427 DOI: 10.1021/acschembio.6b00026 |
0.395 |
|
| 2016 |
Wootten D, Miller LJ, Koole C, Christopoulos A, Sexton PM. Allostery and Biased Agonism at Class B G Protein-Coupled Receptors. Chemical Reviews. PMID 27040440 DOI: 10.1021/acs.chemrev.6b00049 |
0.407 |
|
| 2016 |
Leach K, Gregory KJ, Kufareva I, Khajehali E, Cook AE, Abagyan R, Conigrave AD, Sexton PM, Christopoulos A. Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor. Cell Research. PMID 27002221 DOI: 10.1038/Cr.2016.36 |
0.366 |
|
| 2016 |
Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A. Crystal structures of the M1 and M4 muscarinic acetylcholine receptors. Nature. PMID 26958838 DOI: 10.1038/Nature17188 |
0.597 |
|
| 2016 |
Klein Herenbrink C, Sykes DA, Donthamsetti P, Canals M, Coudrat T, Shonberg J, Scammells PJ, Capuano B, Sexton PM, Charlton SJ, Javitch JA, Christopoulos A, Lane JR. The role of kinetic context in apparent biased agonism at GPCRs. Nature Communications. 7: 10842. PMID 26905976 DOI: 10.1038/Ncomms10842 |
0.4 |
|
| 2016 |
Mistry SN, Lim H, Jörg M, Capuano B, Christopoulos A, Lane JR, Scammells PJ. Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. Acs Chemical Neuroscience. PMID 26891194 DOI: 10.1021/Acschemneuro.6B00018 |
0.481 |
|
| 2016 |
Shang Y, Yeatman HR, Provasi D, Alt A, Christopoulos A, Canals M, Filizola M. Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors. Acs Chemical Biology. PMID 26841170 DOI: 10.1021/Acschembio.5B00712 |
0.437 |
|
| 2016 |
Dong M, Lam PC, Orry A, Sexton PM, Christopoulos A, Abagyan R, Miller LJ. Use of Cysteine Trapping to Map Spatial Approximations between Residues Contributing to the Helix N-capping Motif of Secretin and Distinct Residues within Each of the Extracellular Loops of Its Receptor. The Journal of Biological Chemistry. 291: 5172-84. PMID 26740626 DOI: 10.1074/Jbc.M115.706010 |
0.319 |
|
| 2016 |
De Smet F, Christopoulos A, Carmeliet P. Allosteric targeting of receptor tyrosine kinases. Nature Biotechnology. 32: 1113-20. PMID 25380447 DOI: 10.1038/nbt.3028 |
0.468 |
|
| 2015 |
Desai AJ, Lam PC, Orry A, Abagyan R, Christopoulos A, Sexton PM, Miller LJ. Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex. Journal of Medicinal Chemistry. PMID 26654202 DOI: 10.1021/Acs.Jmedchem.5B01110 |
0.454 |
|
| 2015 |
Mistry SN, Jörg M, Lim H, Vinh NB, Sexton PM, Capuano B, Christopoulos A, Lane JR, Scammells PJ. 4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor. Journal of Medicinal Chemistry. PMID 26624844 DOI: 10.1021/Acs.Jmedchem.5B01562 |
0.58 |
|
| 2015 |
Baltos JA, Gregory KJ, White PJ, Sexton PM, Christopoulos A, May LT. Quantification of Adenosine A1 Receptor Biased Agonism: Implications for Drug Discovery. Biochemical Pharmacology. PMID 26581123 DOI: 10.1016/j.bcp.2015.11.013 |
0.362 |
|
| 2015 |
Mistry SN, Shonberg J, Draper-Joyce CJ, Klein Herenbrink C, Michino M, Shi L, Christopoulos A, Capuano B, Scammells PJ, Lane JR. Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand. Journal of Medicinal Chemistry. 58: 6819-43. PMID 26258690 DOI: 10.1021/Acs.Jmedchem.5B00585 |
0.319 |
|
| 2015 |
Riddy DM, Valant C, Rueda P, Charman WN, Sexton PM, Summers RJ, Christopoulos A, Langmead CJ. Label-Free Kinetics: Exploiting Functional Hemi-Equilibrium to Derive Rate Constants for Muscarinic Receptor Antagonists. Molecular Pharmacology. 88: 779-90. PMID 26243731 DOI: 10.1124/mol.115.100545 |
0.404 |
|
| 2015 |
Shonberg J, Draper-Joyce C, Mistry SN, Christopoulos A, Scammells PJ, Lane JR, Capuano B. Structure-Activity Study of N-((trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a Bitopic Ligand That Acts as a Negative Allosteric Modulator of the Dopamine D2 Receptor. Journal of Medicinal Chemistry. PMID 26052807 DOI: 10.1021/Acs.Jmedchem.5B00581 |
0.364 |
|
| 2015 |
Khajehali E, Malone DT, Glass M, Sexton PM, Christopoulos A, Leach K. Biased Agonism and Biased Allosteric Modulation at the CB1 Cannabinoid Receptor. Molecular Pharmacology. 88: 368-79. PMID 26044547 DOI: 10.1124/mol.115.099192 |
0.418 |
|
| 2015 |
Thompson GL, Lane JR, Coudrat T, Sexton PM, Christopoulos A, Canals M. Biased Agonism of Endogenous Opioid Peptides at the μ-Opioid Receptor. Molecular Pharmacology. 88: 335-46. PMID 26013541 DOI: 10.1124/mol.115.098848 |
0.317 |
|
| 2015 |
Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, et al. Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor. Journal of Medicinal Chemistry. 58: 4220-9. PMID 25901762 DOI: 10.1021/Acs.Jmedchem.5B00007 |
0.487 |
|
| 2015 |
van der Westhuizen ET, Valant C, Sexton PM, Christopoulos A. Endogenous allosteric modulators of G protein-coupled receptors. The Journal of Pharmacology and Experimental Therapeutics. 353: 246-60. PMID 25650376 DOI: 10.1124/jpet.114.221606 |
0.742 |
|
| 2015 |
Koole C, Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM. Differential impact of amino acid substitutions on critical residues of the human glucagon-like peptide-1 receptor involved in peptide activity and small-molecule allostery. The Journal of Pharmacology and Experimental Therapeutics. 353: 52-63. PMID 25630467 DOI: 10.1124/jpet.114.220913 |
0.365 |
|
| 2015 |
Szabo M, Lim HD, Herenbrink CK, Christopoulos A, Lane JR, Capuano B. Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors. Journal of Medicinal Chemistry. 58: 1550-5. PMID 25590655 DOI: 10.1021/jm5013243 |
0.442 |
|
| 2015 |
Dong M, Vattelana AM, Lam PC, Orry AJ, Abagyan R, Christopoulos A, Sexton PM, Haines DR, Miller LJ. Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding. Molecular Pharmacology. 87: 130-40. PMID 25319540 DOI: 10.1124/Mol.114.095430 |
0.389 |
|
| 2014 |
Chen AN, Malone DT, Pabreja K, Sexton PM, Christopoulos A, Canals M. Detection and quantification of allosteric modulation of endogenous m4 muscarinic acetylcholine receptor using impedance-based label-free technology in a neuronal cell line. Journal of Biomolecular Screening. 20: 646-54. PMID 25534830 DOI: 10.1177/1087057114563025 |
0.496 |
|
| 2014 |
Millard CJ, Ludeman JP, Canals M, Bridgford JL, Hinds MG, Clayton DJ, Christopoulos A, Payne RJ, Stone MJ. Structural basis of receptor sulfotyrosine recognition by a CC chemokine: the N-terminal region of CCR3 bound to CCL11/eotaxin-1. Structure (London, England : 1993). 22: 1571-81. PMID 25450766 DOI: 10.1016/J.Str.2014.08.023 |
0.4 |
|
| 2014 |
Abdul-Ridha A, Lane JR, Mistry SN, López L, Sexton PM, Scammells PJ, Christopoulos A, Canals M. Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 289: 33701-11. PMID 25326383 DOI: 10.1074/Jbc.M114.604967 |
0.561 |
|
| 2014 |
Davie BJ, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Development of a photoactivatable allosteric ligand for the m1 muscarinic acetylcholine receptor. Acs Chemical Neuroscience. 5: 902-7. PMID 25188871 DOI: 10.1021/cn500173x |
0.538 |
|
| 2014 |
Lane JR, Donthamsetti P, Shonberg J, Draper-Joyce CJ, Dentry S, Michino M, Shi L, López L, Scammells PJ, Capuano B, Sexton PM, Javitch JA, Christopoulos A. A new mechanism of allostery in a G protein-coupled receptor dimer. Nature Chemical Biology. 10: 745-52. PMID 25108820 DOI: 10.1038/Nchembio.1593 |
0.429 |
|
| 2014 |
Christopoulos A, Changeux JP, Catterall WA, Fabbro D, Burris TP, Cidlowski JA, Olsen RW, Peters JA, Neubig RR, Pin JP, Sexton PM, Kenakin TP, Ehlert FJ, Spedding M, Langmead CJ. International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric ligands. Pharmacological Reviews. 66: 918-47. PMID 25026896 DOI: 10.1124/Pr.114.008862 |
0.465 |
|
| 2014 |
Keov P, López L, Devine SM, Valant C, Lane JR, Scammells PJ, Sexton PM, Christopoulos A. Molecular mechanisms of bitopic ligand engagement with the M1 muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 289: 23817-37. PMID 25006252 DOI: 10.1074/jbc.M114.582874 |
0.513 |
|
| 2014 |
Kruse AC, Kobilka BK, Gautam D, Sexton PM, Christopoulos A, Wess J. Muscarinic acetylcholine receptors: novel opportunities for drug development. Nature Reviews. Drug Discovery. 13: 549-60. PMID 24903776 DOI: 10.1038/Nrd4295 |
0.478 |
|
| 2014 |
Davie BJ, Valant C, White JM, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M â‚ muscarinic acetylcholine receptor. Journal of Medicinal Chemistry. 57: 5405-18. PMID 24856614 DOI: 10.1021/jm500556a |
0.561 |
|
| 2014 |
Schober DA, Croy CH, Xiao H, Christopoulos A, Felder CC. Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites. Molecular Pharmacology. 86: 116-23. PMID 24807966 DOI: 10.1124/Mol.114.091785 |
0.507 |
|
| 2014 |
Croy CH, Schober DA, Xiao H, Quets A, Christopoulos A, Felder CC. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors. Molecular Pharmacology. 86: 106-15. PMID 24807965 DOI: 10.1124/Mol.114.091751 |
0.633 |
|
| 2014 |
Shonberg J, Lopez L, Scammells PJ, Christopoulos A, Capuano B, Lane JR. Biased agonism at G protein-coupled receptors: the promise and the challenges--a medicinal chemistry perspective. Medicinal Research Reviews. 34: 1286-330. PMID 24796277 DOI: 10.1002/med.21318 |
0.455 |
|
| 2014 |
Yeatman HR, Lane JR, Choy KH, Lambert NA, Sexton PM, Christopoulos A, Canals M. Allosteric modulation of M1 muscarinic acetylcholine receptor internalization and subcellular trafficking. The Journal of Biological Chemistry. 289: 15856-66. PMID 24753247 DOI: 10.1074/jbc.M113.536672 |
0.579 |
|
| 2014 |
Langmead CJ, Christopoulos A. Functional and structural perspectives on allosteric modulation of GPCRs. Current Opinion in Cell Biology. 27: 94-101. PMID 24680434 DOI: 10.1016/j.ceb.2013.11.007 |
0.464 |
|
| 2014 |
Valant C, May LT, Aurelio L, Chuo CH, White PJ, Baltos JA, Sexton PM, Scammells PJ, Christopoulos A. Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proceedings of the National Academy of Sciences of the United States of America. 111: 4614-9. PMID 24619092 DOI: 10.1073/pnas.1320962111 |
0.494 |
|
| 2014 |
Abdul-Ridha A, López L, Keov P, Thal DM, Mistry SN, Sexton PM, Lane JR, Canals M, Christopoulos A. Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor. The Journal of Biological Chemistry. 289: 6067-79. PMID 24443568 DOI: 10.1074/Jbc.M113.539080 |
0.508 |
|
| 2014 |
van der Westhuizen ET, Breton B, Christopoulos A, Bouvier M. Quantification of ligand bias for clinically relevant β2-adrenergic receptor ligands: implications for drug taxonomy. Molecular Pharmacology. 85: 492-509. PMID 24366668 DOI: 10.1124/Mol.113.088880 |
0.758 |
|
| 2013 |
Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hübner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 504: 101-6. PMID 24256733 DOI: 10.1038/Nature12735 |
0.497 |
|
| 2013 |
Shonberg J, Herenbrink CK, López L, Christopoulos A, Scammells PJ, Capuano B, Lane JR. A structure-activity analysis of biased agonism at the dopamine D2 receptor. Journal of Medicinal Chemistry. 56: 9199-221. PMID 24138311 DOI: 10.1021/jm401318w |
0.423 |
|
| 2013 |
Dror RO, Green HF, Valant C, Borhani DW, Valcourt JR, Pan AC, Arlow DH, Canals M, Lane JR, Rahmani R, Baell JB, Sexton PM, Christopoulos A, Shaw DE. Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs. Nature. 503: 295-9. PMID 24121438 DOI: 10.1038/Nature12595 |
0.512 |
|
| 2013 |
Koole C, Savage EE, Christopoulos A, Miller LJ, Sexton PM, Wootten D. Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery. Molecular Endocrinology (Baltimore, Md.). 27: 1234-44. PMID 23864649 DOI: 10.1210/me.2013-1116 |
0.319 |
|
| 2013 |
Keov P, Valant C, Devine SM, Lane JR, Scammells PJ, Sexton PM, Christopoulos A. Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor. Molecular Pharmacology. 84: 425-37. PMID 23798605 DOI: 10.1124/mol.113.087320 |
0.44 |
|
| 2013 |
Harikumar KG, Cawston EE, Lam PC, Patil A, Orry A, Henke BR, Abagyan R, Christopoulos A, Sexton PM, Miller LJ. Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor. The Journal of Biological Chemistry. 288: 21082-95. PMID 23754289 DOI: 10.1074/Jbc.M113.480715 |
0.467 |
|
| 2013 |
Mistry SN, Valant C, Sexton PM, Capuano B, Christopoulos A, Scammells PJ. Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. Journal of Medicinal Chemistry. 56: 5151-72. PMID 23718562 DOI: 10.1021/Jm400540B |
0.588 |
|
| 2013 |
Davie BJ, Christopoulos A, Scammells PJ. Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits. Acs Chemical Neuroscience. 4: 1026-48. PMID 23659787 DOI: 10.1021/cn400086m |
0.548 |
|
| 2013 |
Bono F, De Smet F, Herbert C, De Bock K, Georgiadou M, Fons P, Tjwa M, Alcouffe C, Ny A, Bianciotto M, Jonckx B, Murakami M, Lanahan AA, Michielsen C, Sibrac D, ... ... Christopoulos A, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 23: 477-88. PMID 23597562 DOI: 10.1016/J.Ccr.2013.02.019 |
0.362 |
|
| 2013 |
Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM. Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family B G protein-coupled receptor conformations. Proceedings of the National Academy of Sciences of the United States of America. 110: 5211-6. PMID 23479653 DOI: 10.1073/pnas.1221585110 |
0.424 |
|
| 2013 |
Langmead CJ, Christopoulos A. Supra-physiological efficacy at GPCRs: superstition or super agonists? British Journal of Pharmacology. 169: 353-6. PMID 23441648 DOI: 10.1111/bph.12142 |
0.343 |
|
| 2012 |
Harikumar KG, Wootten D, Pinon DI, Koole C, Ball AM, Furness SG, Graham B, Dong M, Christopoulos A, Miller LJ, Sexton PM. Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery. Proceedings of the National Academy of Sciences of the United States of America. 109: 18607-12. PMID 23091034 DOI: 10.1073/pnas.1205227109 |
0.378 |
|
| 2012 |
Willard FS, Wootten D, Showalter AD, Savage EE, Ficorilli J, Farb TB, Bokvist K, Alsina-Fernandez J, Furness SGB, Christopoulos A, Sexton PM, Sloop KW. Small molecule allosteric modulation of the glucagon-like peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin Molecular Pharmacology. 82: 1066-1073. PMID 22930710 DOI: 10.1124/mol.112.080432 |
0.432 |
|
| 2012 |
Sexton PM, Poyner DR, Simms J, Christopoulos A, Hay DL. RAMPs as drug targets. Advances in Experimental Medicine and Biology. 744: 61-74. PMID 22434108 DOI: 10.1007/978-1-4614-2364-5_6 |
0.431 |
|
| 2012 |
Tan JH, Canals M, Ludeman JP, Wedderburn J, Boston C, Butler SJ, Carrick AM, Parody TR, Taleski D, Christopoulos A, Payne RJ, Stone MJ. Design and receptor interactions of obligate dimeric mutant of chemokine monocyte chemoattractant protein-1 (MCP-1). The Journal of Biological Chemistry. 287: 14692-702. PMID 22396538 DOI: 10.1074/Jbc.M111.334201 |
0.352 |
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| 2012 |
Conway RJ, Valant C, Christopoulos A, Robertson AD, Capuano B, Crosby IT. Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT₂C agonists. Bioorganic & Medicinal Chemistry Letters. 22: 2560-4. PMID 22381048 DOI: 10.1016/j.bmcl.2012.01.122 |
0.356 |
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| 2012 |
Valant C, Aurelio L, Devine SM, Ashton TD, White JM, Sexton PM, Christopoulos A, Scammells PJ. Synthesis and characterization of novel 2-amino-3-benzoylthiophene derivatives as biased allosteric agonists and modulators of the adenosine A(1) receptor. Journal of Medicinal Chemistry. 55: 2367-75. PMID 22315963 DOI: 10.1021/jm201600e |
0.398 |
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| 2012 |
Leach K, Simms J, Sexton PM, Christopoulos A. Structure-function studies of muscarinic acetylcholine receptors. Handbook of Experimental Pharmacology. 29-48. PMID 22222693 DOI: 10.1007/978-3-642-23274-9_2 |
0.474 |
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| 2012 |
Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW. Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. Journal of Medicinal Chemistry. 55: 1445-64. PMID 22148748 DOI: 10.1021/Jm201139R |
0.465 |
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| 2012 |
Koole C, Wootten D, Simms J, Miller LJ, Christopoulos A, Sexton PM. Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) has a critical role in GLP-1 peptide binding and receptor activation. The Journal of Biological Chemistry. 287: 3642-58. PMID 22147710 DOI: 10.1074/jbc.M111.309328 |
0.405 |
|
| 2012 |
Koole C, Wootten D, Simms J, Savage EE, Miller LJ, Christopoulos A, Sexton PM. Second extracellular loop of human glucagon-like peptide-1 receptor (GLP-1R) differentially regulates orthosteric but not allosteric agonist binding and function. The Journal of Biological Chemistry. 287: 3659-73. PMID 22147709 DOI: 10.1074/jbc.M111.309369 |
0.345 |
|
| 2012 |
Canals M, Lane JR, Wen A, Scammells PJ, Sexton PM, Christopoulos A. A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation. The Journal of Biological Chemistry. 287: 650-659. PMID 22086918 DOI: 10.1074/jbc.M111.314278 |
0.564 |
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| 2012 |
Valant C, Felder CC, Sexton PM, Christopoulos A. Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects. Molecular Pharmacology. 81: 41-52. PMID 21989256 DOI: 10.1124/Mol.111.074872 |
0.578 |
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| 2011 |
Kenakin T, Watson C, Muniz-Medina V, Christopoulos A, Novick S. A simple method for quantifying functional selectivity and agonist bias. Acs Chemical Neuroscience. 3: 193-203. PMID 22860188 DOI: 10.1021/cn200111m |
0.43 |
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| 2011 |
Stallaert W, Christopoulos A, Bouvier M. Ligand functional selectivity and quantitative pharmacology at G protein-coupled receptors. Expert Opinion On Drug Discovery. 6: 811-25. PMID 22651124 DOI: 10.1517/17460441.2011.586691 |
0.557 |
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| 2011 |
Koole C, Wootten D, Simms J, Valant C, Miller LJ, Christopoulos A, Sexton PM. Polymorphism and ligand dependent changes in human glucagon-like peptide-1 receptor (GLP-1R) function: allosteric rescue of loss of function mutation. Molecular Pharmacology. 80: 486-97. PMID 21616920 DOI: 10.1124/mol.111.072884 |
0.371 |
|
| 2011 |
Bosnyak S, Jones ES, Christopoulos A, Aguilar MI, Thomas WG, Widdop RE. Relative affinity of angiotensin peptides and novel ligands at AT1 and AT2 receptors. Clinical Science (London, England : 1979). 121: 297-303. PMID 21542804 DOI: 10.1042/CS20110036 |
0.362 |
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| 2011 |
Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A. The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor. Molecular Pharmacology. 79: 855-65. PMID 21300722 DOI: 10.1124/Mol.111.070938 |
0.507 |
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| 2011 |
Evans BA, Broxton N, Merlin J, Sato M, Hutchinson DS, Christopoulos A, Summers RJ. Quantification of functional selectivity at the human α(1A)-adrenoceptor. Molecular Pharmacology. 79: 298-307. PMID 20978120 DOI: 10.1124/mol.110.067454 |
0.325 |
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| 2010 |
Gregory KJ, Sexton PM, Christopoulos A. Overview of receptor allosterism Current Protocols in Pharmacology / Editorial Board, S.J. Enna (Editor-in-Chief) ... [Et Al.]. PMID 21935895 DOI: 10.1002/0471141755.ph0121s51 |
0.467 |
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| 2010 |
Wootten DL, Simms J, Hay DL, Christopoulos A, Sexton PM. Receptor activity modifying proteins and their potential as drug targets. Progress in Molecular Biology and Translational Science. 91: 53-79. PMID 20691959 DOI: 10.1016/S1877-1173(10)91003-X |
0.385 |
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| 2010 |
Valant C, Aurelio L, Urmaliya VB, White P, Scammells PJ, Sexton PM, Christopoulos A. Delineating the mode of action of adenosine A1 receptor allosteric modulators. Molecular Pharmacology. 78: 444-55. PMID 20547736 DOI: 10.1124/mol.110.064568 |
0.455 |
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| 2010 |
Koole C, Wootten D, Simms J, Valant C, Sridhar R, Woodman OL, Miller LJ, Summers RJ, Christopoulos A, Sexton PM. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: implications for drug screening. Molecular Pharmacology. 78: 456-65. PMID 20547734 DOI: 10.1124/mol.110.065664 |
0.306 |
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| 2010 |
Avlani VA, Langmead CJ, Guida E, Wood MD, Tehan BG, Herdon HJ, Watson JM, Sexton PM, Christopoulos A. Orthosteric and allosteric modes of interaction of novel selective agonists of the M1 muscarinic acetylcholine receptor. Molecular Pharmacology. 78: 94-104. PMID 20413650 DOI: 10.1124/mol.110.064345 |
0.507 |
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| 2010 |
Nawaratne V, Leach K, Felder CC, Sexton PM, Christopoulos A. Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms. The Journal of Biological Chemistry. 285: 19012-21. PMID 20406819 DOI: 10.1074/Jbc.M110.125096 |
0.579 |
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| 2010 |
van der Westhuizen ET, Christopoulos A, Sexton PM, Wade JD, Summers RJ. H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3). Molecular Pharmacology. 77: 759-72. PMID 20159943 DOI: 10.1124/mol.109.061432 |
0.677 |
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| 2010 |
Gregory KJ, Hall NE, Tobin AB, Sexton PM, Christopoulos A. Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias. The Journal of Biological Chemistry. 285: 7459-74. PMID 20051519 DOI: 10.1074/jbc.M109.094011 |
0.516 |
|
| 2010 |
Leach K, Loiacono RE, Felder CC, McKinzie DL, Mogg A, Shaw DB, Sexton PM, Christopoulos A. Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 35: 855-69. PMID 19940843 DOI: 10.1038/Npp.2009.194 |
0.584 |
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| 2009 |
Aurelio L, Valant C, Figler H, Flynn BL, Linden J, Sexton PM, Christopoulos A, Scammells PJ. 3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists. Bioorganic & Medicinal Chemistry. 17: 7353-61. PMID 19751980 DOI: 10.1016/J.Bmc.2009.08.024 |
0.325 |
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| 2009 |
Stewart GD, Valant C, Dowell SJ, Mijaljica D, Devenish RJ, Scammells PJ, Sexton PM, Christopoulos A. Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity. The Journal of Pharmacology and Experimental Therapeutics. 331: 277-86. PMID 19641164 DOI: 10.1124/jpet.109.158667 |
0.417 |
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| 2009 |
Aurelio L, Valant C, Flynn BL, Sexton PM, Christopoulos A, Scammells PJ. Allosteric modulators of the adenosine A1 receptor: synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes. Journal of Medicinal Chemistry. 52: 4543-7. PMID 19514747 DOI: 10.1021/jm9002582 |
0.315 |
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| 2009 |
Gao F, Harikumar KG, Dong M, Lam PC, Sexton PM, Christopoulos A, Bordner A, Abagyan R, Miller LJ. Functional importance of a structurally distinct homodimeric complex of the family B G protein-coupled secretin receptor. Molecular Pharmacology. 76: 264-74. PMID 19429716 DOI: 10.1124/Mol.109.055756 |
0.387 |
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| 2009 |
Sexton PM, Poyner DR, Simms J, Christopoulos A, Hay DL. Modulating receptor function through RAMPs: can they represent drug targets in themselves? Drug Discovery Today. 14: 413-9. PMID 19150656 DOI: 10.1016/j.drudis.2008.12.009 |
0.451 |
|
| 2009 |
Conn PJ, Christopoulos A, Lindsley CW. Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nature Reviews. Drug Discovery. 8: 41-54. PMID 19116626 DOI: 10.1038/Nrd2760 |
0.461 |
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| 2009 |
Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E. Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. The Journal of Pharmacology and Experimental Therapeutics. 328: 893-9. PMID 19029429 DOI: 10.1124/jpet.108.145508 |
0.453 |
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| 2009 |
Antony J, Kellershohn K, Mohr-Andrä M, Kebig A, Prilla S, Muth M, Heller E, Disingrini T, Dallanoce C, Bertoni S, Schrobang J, Tränkle C, Kostenis E, Christopoulos A, Höltje HD, et al. Dualsteric GPCR targeting: a novel route to binding and signaling pathway selectivity. Faseb Journal : Official Publication of the Federation of American Societies For Experimental Biology. 23: 442-50. PMID 18842964 DOI: 10.1096/fj.08-114751 |
0.574 |
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| 2008 |
Ferguson GN, Valant C, Horne J, Figler H, Flynn BL, Linden J, Chalmers DK, Sexton PM, Christopoulos A, Scammells PJ. 2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists. Journal of Medicinal Chemistry. 51: 6165-72. PMID 18771255 DOI: 10.1021/Jm800557D |
0.426 |
|
| 2008 |
Valant C, Gregory KJ, Hall NE, Scammells PJ, Lew MJ, Sexton PM, Christopoulos A. A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. The Journal of Biological Chemistry. 283: 29312-21. PMID 18723515 DOI: 10.1074/jbc.M803801200 |
0.592 |
|
| 2008 |
Nawaratne V, Leach K, Suratman N, Loiacono RE, Felder CC, Armbruster BN, Roth BL, Sexton PM, Christopoulos A. New insights into the function of M4 muscarinic acetylcholine receptors gained using a novel allosteric modulator and a DREADD (designer receptor exclusively activated by a designer drug). Molecular Pharmacology. 74: 1119-31. PMID 18628403 DOI: 10.1124/Mol.108.049353 |
0.6 |
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| 2008 |
Gao F, Sexton PM, Christopoulos A, Miller LJ. Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor. Bioorganic & Medicinal Chemistry Letters. 18: 4401-4. PMID 18621527 DOI: 10.1016/j.bmcl.2008.06.053 |
0.443 |
|
| 2008 |
Morfis M, Tilakaratne N, Furness SG, Christopoulos G, Werry TD, Christopoulos A, Sexton PM. Receptor activity-modifying proteins differentially modulate the G protein-coupling efficiency of amylin receptors. Endocrinology. 149: 5423-31. PMID 18599553 DOI: 10.1210/en.2007-1735 |
0.429 |
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| 2008 |
Qi T, Christopoulos G, Bailey RJ, Christopoulos A, Sexton PM, Hay DL. Identification of N-terminal receptor activity-modifying protein residues important for calcitonin gene-related peptide, adrenomedullin, and amylin receptor function. Molecular Pharmacology. 74: 1059-71. PMID 18593822 DOI: 10.1124/mol.108.047142 |
0.408 |
|
| 2008 |
Udawela M, Christopoulos G, Morfis M, Tilakaratne N, Christopoulos A, Sexton PM. The effects of C-terminal truncation of receptor activity modifying proteins on the induction of amylin receptor phenotype from human CTb receptors. Regulatory Peptides. 145: 65-71. PMID 17884192 DOI: 10.1016/j.regpep.2007.08.003 |
0.445 |
|
| 2007 |
Avlani VA, Gregory KJ, Morton CJ, Parker MW, Sexton PM, Christopoulos A. Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands Journal of Biological Chemistry. 282: 25677-25686. PMID 17591774 DOI: 10.1074/jbc.M702311200 |
0.354 |
|
| 2007 |
May LT, Avlani VA, Langmead CJ, Herdon HJ, Wood MD, Sexton PM, Christopoulos A. Structure-function studies of allosteric agonism at M2 muscarinic acetylcholine receptors. Molecular Pharmacology. 72: 463-76. PMID 17525129 DOI: 10.1124/mol.107.037630 |
0.499 |
|
| 2007 |
Urban JD, Clarke WP, von Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA, Roth BL, Christopoulos A, Sexton PM, Miller KJ, Spedding M, Mailman RB. Functional selectivity and classical concepts of quantitative pharmacology. The Journal of Pharmacology and Experimental Therapeutics. 320: 1-13. PMID 16803859 DOI: 10.1124/Jpet.106.104463 |
0.469 |
|
| 2006 |
Hay DL, Christopoulos G, Christopoulos A, Sexton PM. Determinants of 1-piperidinecarboxamide, N-[2-[[5-amino-l-[[4-(4-pyridinyl)-l-piperazinyl]carbonyl]pentyl]amino]-1-[(3,5-dibromo-4-hydroxyphenyl)methyl]-2-oxoethyl]-4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl) (BIBN4096BS) affinity for calcitonin gene-related peptide and amylin receptors--the role of receptor activity modifying protein 1. Molecular Pharmacology. 70: 1984-91. PMID 16959943 DOI: 10.1124/mol.106.027953 |
0.396 |
|
| 2006 |
Langmead CJ, Christopoulos A. Allosteric agonists of 7TM receptors: expanding the pharmacological toolbox. Trends in Pharmacological Sciences. 27: 475-81. PMID 16889837 DOI: 10.1016/j.tips.2006.07.009 |
0.475 |
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| 2006 |
Sexton PM, Morfis M, Tilakaratne N, Hay DL, Udawela M, Christopoulos G, Christopoulos A. Complexing receptor pharmacology: modulation of family B G protein-coupled receptor function by RAMPs. Annals of the New York Academy of Sciences. 1070: 90-104. PMID 16888151 DOI: 10.1196/annals.1317.076 |
0.39 |
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| 2006 |
Mathiesen JM, Christopoulos A, Ulven T, Royer JF, Campillo M, Heinemann A, Pardo L, Kostenis E. On the mechanism of interaction of potent surmountable and insurmountable antagonists with the prostaglandin D2 receptor CRTH2. Molecular Pharmacology. 69: 1441-53. PMID 16418339 DOI: 10.1124/Mol.105.017681 |
0.412 |
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| 2006 |
Langmead CJ, Fry VA, Forbes IT, Branch CL, Christopoulos A, Wood MD, Herdon HJ. Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist. Molecular Pharmacology. 69: 236-46. PMID 16207821 DOI: 10.1124/mol.105.017814 |
0.508 |
|
| 2005 |
Price MR, Baillie GL, Thomas A, Stevenson LA, Easson M, Goodwin R, McLean A, McIntosh L, Goodwin G, Walker G, Westwood P, Marrs J, Thomson F, Cowley P, Christopoulos A, et al. Allosteric modulation of the cannabinoid CB1 receptor. Molecular Pharmacology. 68: 1484-95. PMID 16113085 DOI: 10.1124/Mol.105.016162 |
0.381 |
|
| 2005 |
Werry TD, Gregory KJ, Sexton PM, Christopoulos A. Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2 Journal of Neurochemistry. 93: 1603-1615. PMID 15935077 DOI: 10.1111/j.1471-4159.2005.03161.x |
0.34 |
|
| 2005 |
Kostenis E, Milligan G, Christopoulos A, Sanchez-Ferrer CF, Heringer-Walther S, Sexton PM, Gembardt F, Kellett E, Martini L, Vanderheyden P, Schultheiss HP, Walther T. G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor. Circulation. 111: 1806-13. PMID 15809376 DOI: 10.1161/01.Cir.0000160867.23556.7D |
0.322 |
|
| 2005 |
Hay DL, Christopoulos G, Christopoulos A, Poyner DR, Sexton PM. Pharmacological discrimination of calcitonin receptor: receptor activity-modifying protein complexes. Molecular Pharmacology. 67: 1655-65. PMID 15692146 DOI: 10.1124/mol.104.008615 |
0.319 |
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| 2004 |
Devlin MG, Smith NJ, Ryan OM, Guida E, Sexton PM, Christopoulos A. Regulation of serotonin 5-HT2C receptors by chronic ligand exposure. European Journal of Pharmacology. 498: 59-69. PMID 15363976 DOI: 10.1016/j.ejphar.2004.07.102 |
0.302 |
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| 2004 |
May LT, Lin Y, Sexton PM, Christopoulos A. Regulation of M2 muscarinic acetylcholine receptor expression and signaling by prolonged exposure to allosteric modulators. The Journal of Pharmacology and Experimental Therapeutics. 312: 382-90. PMID 15333678 DOI: 10.1124/JPET.104.073767 |
0.505 |
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| 2003 |
Christopoulos A, Christopoulos G, Morfis M, Udawela M, Laburthe M, Couvineau A, Kuwasako K, Tilakaratne N, Sexton PM. Novel receptor partners and function of receptor activity-modifying proteins. The Journal of Biological Chemistry. 278: 3293-7. PMID 12446722 DOI: 10.1074/jbc.C200629200 |
0.417 |
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| 2002 |
Lyon GJ, Wright JS, Christopoulos A, Novick RP, Muir TW. Reversible and specific extracellular antagonism of receptor-histidine kinase signaling. The Journal of Biological Chemistry. 277: 6247-53. PMID 11733525 DOI: 10.1074/Jbc.M109989200 |
0.383 |
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