Year |
Citation |
Score |
2023 |
Beretta M, Dai Y, Olzomer EM, Vancuylenburg CS, Santiago-Rivera JA, Philp AM, Hargett SR, Li K, Shah DP, Chen SY, Alexopoulos SJ, Li C, Harris TE, Lee B, Wathier M, ... ... Santos WL, et al. Liver-selective imidazolopyrazine mitochondrial uncoupler SHD865 reverses adiposity and glucose intolerance in mice. Diabetes. PMID 37870907 DOI: 10.2337/db23-0233 |
0.645 |
|
2023 |
Shrader CW, Foster D, Kharel Y, Huang T, Lynch KR, Santos WL. Imidazole-based sphingosine-1-phosphate transporter Spns2 inhibitors. Bioorganic & Medicinal Chemistry Letters. 129516. PMID 37832799 DOI: 10.1016/j.bmcl.2023.129516 |
0.312 |
|
2023 |
Kharel Y, Huang T, Santos WL, Lynch KR. Assay of Sphingosine 1-phosphate Transporter Spinster Homolog 2 (Spns2) Inhibitors. Slas Discovery : Advancing Life Sciences R & D. PMID 37454972 DOI: 10.1016/j.slasd.2023.07.001 |
0.305 |
|
2023 |
Burgio AL, Shrader CW, Kharel Y, Huang T, Salamoun JM, Lynch KR, Santos WL. 2-Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spinster Homolog 2 (Spns2). Journal of Medicinal Chemistry. PMID 37010497 DOI: 10.1021/acs.jmedchem.3c00149 |
0.338 |
|
2023 |
Li H, Ehnstrom J, Milton M, Santos W, Zell M, Dai Y. Identification and enrichment of a UV-induced degradant of Anagrelide drug substance. Journal of Pharmaceutical and Biomedical Analysis. 229: 115352. PMID 36989665 DOI: 10.1016/j.jpba.2023.115352 |
0.654 |
|
2022 |
Dye KJ, Vogelaar NJ, O'Hara M, Sobrado P, Santos W, Carlier PR, Yang Z. Discovery of Two Inhibitors of the Type IV Pilus Assembly ATPase PilB as Potential Antivirulence Compounds. Microbiology Spectrum. e0387722. PMID 36377931 DOI: 10.1128/spectrum.03877-22 |
0.572 |
|
2022 |
Dai Y, Santiago-Rivera JA, Hargett S, Salamoun JM, Hoehn KL, Santos WL. Conversion of oxadiazolo[3,4-b]pyrazines to imidazo[4,5-b]pyrazines via a tandem reduction-cyclization sequence generates new mitochondrial uncouplers. Bioorganic & Medicinal Chemistry Letters. 73: 128912. PMID 35907607 DOI: 10.1016/j.bmcl.2022.128912 |
0.65 |
|
2022 |
Fritzemeier R, Foster D, Peralta A, Payette M, Kharel Y, Huang T, Lynch KR, Santos WL. Discovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors. Journal of Medicinal Chemistry. PMID 35609189 DOI: 10.1021/acs.jmedchem.1c02171 |
0.318 |
|
2020 |
Li H, Sibley CD, Kharel Y, Huang T, Brown AM, Wonilowicz LG, Bevan DR, Lynch KR, Santos WL. Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors. Bioorganic & Medicinal Chemistry. 30: 115941. PMID 33385956 DOI: 10.1016/j.bmc.2020.115941 |
0.354 |
|
2020 |
Grams RJ, Garcia CJ, Szwetkowski C, Santos WL. Catalytic, Transition-Metal-Free Semireduction of Propiolamide Derivatives: Scope and Mechanistic Investigation. Organic Letters. PMID 32846095 DOI: 10.1021/Acs.Orglett.0C02567 |
0.31 |
|
2020 |
Salamoun J, Garcia CJ, Hargett S, Murray J, Chen SY, Baretta M, Alexopoulos S, Shah D, Olzomer E, Tucker S, Hoehn K, Santos WL. 6-Amino-[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol Derivatives as Efficacious Mitochondrial Uncouplers in STAM Mouse Model of Non-alcoholic Steatohepatitis. Journal of Medicinal Chemistry. PMID 32392051 DOI: 10.1021/Acs.Jmedchem.0C00542 |
0.306 |
|
2020 |
Liu X, Ming W, Luo X, Friedrich A, Maier J, Radius U, Santos WL, Marder TB. Regio- and Stereoselective Synthesis of 1,1-Diborylalkenes via Brønsted Base-Catalyzed Mixed Diboration of Alkynyl Esters and Amides with BpinBdan. European Journal of Organic Chemistry. 2020: 1941-1946. PMID 32362780 DOI: 10.1002/Ejoc.202000128 |
0.306 |
|
2020 |
Kharel Y, Huang T, Salamon A, Harris T, Santos WL, Lynch KR. Mechanism of sphingosine 1-phosphate clearance from blood. The Biochemical Journal. PMID 32065229 DOI: 10.1042/Bcj20190730 |
0.36 |
|
2020 |
Childress ES, Salamoun J, Hargett S, Alexopoulos S, Chen SY, Shah DP, Santiago-Rivera J, Garcia C, Dai Y, Tucker SP, Hoehn K, Santos WL. [1,2,5]Oxadiazolo[3,4-b]pyrazine-5,6-diamine Derivatives as Mitochondrial Uncouplers for the Potential Treatment of Nonalcoholic Steatohepatitis. Journal of Medicinal Chemistry. PMID 32017849 DOI: 10.1021/Acs.Jmedchem.9B01440 |
0.687 |
|
2020 |
Sibley CD, Morris EA, Kharel Y, Brown AM, Bevan DR, Lynch KR, Santos WL. Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity. Journal of Medicinal Chemistry. PMID 31895563 DOI: 10.1021/Acs.Jmedchem.9B01508 |
0.325 |
|
2019 |
Peralta AN, Dai Y, Sherpa C, Le Grice SFJ, Santos WL. Molecular recognition of HIV-1 RNAs with branched peptides. Methods in Enzymology. 623: 373-400. PMID 31239054 DOI: 10.1016/Bs.Mie.2019.04.021 |
0.674 |
|
2019 |
Dai Y, Peralta AN, Wynn JE, Sherpa C, Li H, Verma A, Le Grice SFJ, Santos WL. Molecular recognition of a branched peptide with HIV-1 Rev Response Element (RRE) RNA. Bioorganic & Medicinal Chemistry. PMID 30879859 DOI: 10.1016/J.Bmc.2019.03.016 |
0.686 |
|
2019 |
Worrell BL, Brown AM, Santos WL, Bevan DR. In silico Characterization of Structural Distinctions Between Isoforms of Human and Mouse Sphingosine Kinases for Accelerating Drug Discovery. Journal of Chemical Information and Modeling. PMID 30844267 DOI: 10.1021/Acs.Jcim.8B00931 |
0.343 |
|
2018 |
Dai Y, Wynn J, Peralta A, Sherpa C, Jayaraman B, Li H, Verma A, Frankel AD, Le Grice SFJ, Santos WL. Discovery of a Branched Peptide that Recognizes the Rev Response Element (RRE) RNA and Blocks HIV-1 Replication. Journal of Medicinal Chemistry. PMID 30289719 DOI: 10.1021/Acs.Jmedchem.8B01076 |
0.684 |
|
2018 |
Fritzemeier R, Gates A, Guo X, Lin Z, Santos WL. Transition metal-free trans hydroboration of alkynoic acid derivatives: Experimental and theoretical studies. The Journal of Organic Chemistry. PMID 29986587 DOI: 10.1021/Acs.Joc.8B01493 |
0.303 |
|
2018 |
Kharel Y, Agah S, Huang T, Mendelson AJ, Eletu OT, Barkey-Bircann P, Gesualdi J, Smith JS, Santos WL, Lynch KR. Saccharomyces cerevisiae as a platform for assessing sphingolipid lipid kinase inhibitors. Plos One. 13: e0192179. PMID 29672528 DOI: 10.1371/Journal.Pone.0192179 |
0.381 |
|
2017 |
Childress ES, Kharel Y, Brown AM, Bevan DR, Lynch KR, Santos WL. Transforming Sphingosine Kinase 1 Inhibitors into Dual and Sphingosine Kinase 2 Selective Inhibitors: Design, Synthesis, and In Vivo Activity. Journal of Medicinal Chemistry. PMID 28406646 DOI: 10.1021/Acs.Jmedchem.7B00233 |
0.327 |
|
2017 |
Verma A, Snead RF, Dai Y, Slebodnick C, Yang Y, Yu H, Yao F, Santos WL. Substrate-Assisted, Transition-Metal-Free Diboration of Alkynamides with Mixed Diboron: Regio- and Stereoselective Access to trans-1,2-Vinyldiboronates. Angewandte Chemie (International Ed. in English). PMID 28371182 DOI: 10.1002/Anie.201700946 |
0.657 |
|
2016 |
Valenciano AL, Ramsey AC, Santos WL, Mackey ZB. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorganic & Medicinal Chemistry. PMID 27519462 DOI: 10.1016/J.Bmc.2016.07.069 |
0.304 |
|
2016 |
Wynn JE, Zhang W, Tebit DM, Gray LR, Hammarskjold ML, Rekosh D, Santos WL. Effect of intercalator and Lewis acid-base branched peptide complex formation: boosting affinity towards HIV-1 RRE RNA. Medchemcomm. 7: 1436-1440. PMID 27453773 DOI: 10.1039/C6Md00171H |
0.309 |
|
2016 |
Wynn JE, Zhang W, Tebit DM, Gray LR, Hammarskjold ML, Rekosh D, Santos WL. Characterization and in vitro activity of a branched peptide boronic acid that interacts with HIV-1 RRE RNA. Bioorganic & Medicinal Chemistry. PMID 27091070 DOI: 10.1016/J.Bmc.2016.04.009 |
0.325 |
|
2015 |
Congdon MD, Childress ES, Patwardhan NN, Gumkowski J, Morris EA, Kharel Y, Lynch KR, Santos WL. Structure-activity relationship studies of the lipophilic tail region of sphingosine kinase 2 inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 25862200 DOI: 10.1016/J.Bmcl.2015.03.041 |
0.315 |
|
2015 |
Patwardhan NN, Morris EA, Kharel Y, Raje MR, Gao M, Tomsig JL, Lynch KR, Santos WL. Structure-activity relationship studies and in vivo activity of guanidine-based sphingosine kinase inhibitors: discovery of SphK1- and SphK2-selective inhibitors. Journal of Medicinal Chemistry. 58: 1879-99. PMID 25643074 DOI: 10.1021/Jm501760D |
0.335 |
|
2015 |
Santos WL, Lynch KR. Drugging sphingosine kinases. Acs Chemical Biology. 10: 225-33. PMID 25384187 DOI: 10.1021/Cb5008426 |
0.303 |
|
2013 |
Zhang W, Bryson DI, Crumpton JB, Wynn J, Santos WL. Targeting folded RNA: a branched peptide boronic acid that binds to a large surface area of HIV-1 RRE RNA. Organic & Biomolecular Chemistry. 11: 6263-71. PMID 23925474 DOI: 10.1039/C3Ob41053F |
0.319 |
|
2013 |
Zhang W, Bryson DI, Crumpton JB, Wynn J, Santos WL. Branched peptide boronic acids (BPBAs): a novel mode of binding towards RNA. Chemical Communications (Cambridge, England). 49: 2436-8. PMID 23412370 DOI: 10.1039/C3Cc00243H |
0.309 |
|
2012 |
Gude L, Berkovitch SS, Santos WL, Kutchukian PS, Pawloski AR, Kuimelis R, McGall G, Verdine GL. Mapping targetable sites on human telomerase RNA pseudoknot/template domain using 2'-OMe RNA-interacting polynucleotide (RIPtide) microarrays. The Journal of Biological Chemistry. 287: 18843-53. PMID 22451672 DOI: 10.1074/Jbc.M111.316596 |
0.532 |
|
2012 |
Raje MR, Knott K, Kharel Y, Bissel P, Lynch KR, Santos WL. Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors. Bioorganic & Medicinal Chemistry. 20: 183-94. PMID 22137932 DOI: 10.1016/J.Bmc.2011.11.011 |
0.307 |
|
2010 |
Knott K, Fishovitz J, Thorpe SB, Lee I, Santos WL. N-Terminal peptidic boronic acids selectively inhibit human ClpXP. Organic & Biomolecular Chemistry. 8: 3451-6. PMID 20523950 DOI: 10.1039/C004247A |
0.306 |
|
2008 |
Komazin-Meredith G, Petrella RJ, Santos WL, Filman DJ, Hogle JM, Verdine GL, Karplus M, Coen DM. The human cytomegalovirus UL44 C clamp wraps around DNA. Structure (London, England : 1993). 16: 1214-25. PMID 18682223 DOI: 10.1016/J.Str.2008.05.008 |
0.503 |
|
2008 |
Komazin-Meredith G, Santos WL, Filman DJ, Hogle JM, Verdine GL, Coen DM. The positively charged surface of herpes simplex virus UL42 mediates DNA binding. The Journal of Biological Chemistry. 283: 6154-61. PMID 18178550 DOI: 10.1074/Jbc.M708691200 |
0.517 |
|
2008 |
Zhao Z, McKee CJ, Kessl JJ, Santos WL, Daigle JE, Engelman A, Verdine G, Kvaratskhelia M. Subunit-specific protein footprinting reveals significant structural rearrangements and a role for N-terminal Lys-14 of HIV-1 Integrase during viral DNA binding. The Journal of Biological Chemistry. 283: 5632-41. PMID 18093980 DOI: 10.1074/Jbc.M705241200 |
0.54 |
|
2006 |
Banerjee A, Santos WL, Verdine GL. Structure of a DNA glycosylase searching for lesions. Science (New York, N.Y.). 311: 1153-7. PMID 16497933 DOI: 10.1126/Science.1120288 |
0.567 |
|
2006 |
Johnson AA, Santos W, Pais GC, Marchand C, Amin R, Burke TR, Verdine G, Pommier Y. Integration requires a specific interaction of the donor DNA terminal 5'-cytosine with glutamine 148 of the HIV-1 integrase flexible loop. The Journal of Biological Chemistry. 281: 461-7. PMID 16257967 DOI: 10.1074/Jbc.M511348200 |
0.534 |
|
2004 |
Santos WL, Heasley BH, Jarosz R, Carter KM, Lynch KR, Macdonald TL. Synthesis and biological evaluation of phosphonic and thiophosphoric acid derivatives of lysophosphatidic acid. Bioorganic & Medicinal Chemistry Letters. 14: 3473-6. PMID 15177455 DOI: 10.1016/J.Bmcl.2004.04.061 |
0.752 |
|
2002 |
Kapetanovic IM, Torchin CD, Strong JM, Yonekawa WD, Lu C, Li AP, Dieckhaus CM, Santos WL, Macdonald TL, Sofia RD, Kupferberg HJ. Reactivity of atropaldehyde, a felbamate metabolite in human liver tissue in vitro Chemico-Biological Interactions. 142: 119-134. PMID 12399159 DOI: 10.1016/S0009-2797(02)00058-3 |
0.77 |
|
2002 |
Roller SG, Dieckhaus CM, Santos WL, Sofia RD, Macdonald TL. Interaction between human serum albumin and the felbamate metabolites 4-Hydroxy-5-phenyl-[1,3]oxazinan-2-one and 2-phenylpropenal. Chemical Research in Toxicology. 15: 815-24. PMID 12067249 DOI: 10.1021/Tx025509H |
0.745 |
|
2002 |
Roller SG, Dieckhaus CM, Santos WL, Sofia RD, Macdonald TL. Interaction between human serum albumin and the felbamate metabolites 4-hydroxy-5-phenyl-[1,3]oxazinan-2-one and 2-phenylpropenal Chemical Research in Toxicology. 15: 815-824. DOI: 10.1021/tx025509h |
0.722 |
|
2001 |
Heise CE, Santos WL, Schreihofer AM, Heasley BH, Mukhin YV, Macdonald TL, Lynch KR. Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Molecular Pharmacology. 60: 1173-80. PMID 11723223 DOI: 10.1124/Mol.60.6.1173 |
0.755 |
|
2001 |
Dieckhaus CM, Santos WL, Sofia RD, Macdonald TL. The chemistry, toxicology, and identification in rat and human urine of 4-hydroxy-5-phenyl-1,3-oxazaperhydroin-2-one: A reactive metabolite in felbamate bioactivation Chemical Research in Toxicology. 14: 958-964. PMID 11511169 DOI: 10.1021/Tx000139N |
0.768 |
|
2001 |
Dieckhaus CM, Roller SG, Santos WL, Sofia RD, Macdonald TL. Role of glutathione S-transferases A1-1, M1-1, and P1-1 in the detoxification of 2-phenylpropenal, a reactive felbamate metabolite Chemical Research in Toxicology. 14: 511-516. PMID 11368548 DOI: 10.1021/Tx000141E |
0.728 |
|
2001 |
Hooks SB, Santos WL, Im DS, Heise CE, Macdonald TL, Lynch KR. Lysophosphatidic acid-induced mitogenesis is regulated by lipid phosphate phosphatases and is Edg-receptor independent. The Journal of Biological Chemistry. 276: 4611-21. PMID 11042183 DOI: 10.1074/Jbc.M007782200 |
0.531 |
|
2000 |
Santos WL, Rossi JA, Boggs SD, MacDonald TL. The molecular pharmacology of lysophosphatidate signaling. Annals of the New York Academy of Sciences. 905: 232-41. PMID 10818457 DOI: 10.1111/J.1749-6632.2000.Tb06553.X |
0.474 |
|
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