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Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM. McDaniel KF, et al. Among authors: gao w. J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12. J Med Chem. 2017. PMID: 28949521
Highlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530).
Wagner R, Randolph JT, Patel SV, Nelson L, Matulenko MA, Keddy R, Pratt JK, Liu D, Krueger AC, Donner PL, Hutchinson DK, Flentge C, Betebenner D, Rockway T, Maring CJ, Ng TI, Krishnan P, Pilot-Matias T, Collins C, Panchal N, Reisch T, Dekhtyar T, Mondal R, Stolarik DF, Gao Y, Gao W, Beno DA, Kati WM. Wagner R, et al. Among authors: gao w, gao y. J Med Chem. 2018 May 10;61(9):4052-4066. doi: 10.1021/acs.jmedchem.8b00082. Epub 2018 Apr 23. J Med Chem. 2018. PMID: 29653491
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor.
Wang L, Doherty GA, Judd AS, Tao ZF, Hansen TM, Frey RR, Song X, Bruncko M, Kunzer AR, Wang X, Wendt MD, Flygare JA, Catron ND, Judge RA, Park CH, Shekhar S, Phillips DC, Nimmer P, Smith ML, Tahir SK, Xiao Y, Xue J, Zhang H, Le PN, Mitten MJ, Boghaert ER, Gao W, Kovar P, Choo EF, Diaz D, Fairbrother WJ, Elmore SW, Sampath D, Leverson JD, Souers AJ. Wang L, et al. Among authors: gao w. ACS Med Chem Lett. 2020 Mar 30;11(10):1829-1836. doi: 10.1021/acsmedchemlett.9b00568. eCollection 2020 Oct 8. ACS Med Chem Lett. 2020. PMID: 33062160 Free PMC article.
Discovery of 4-[(2R,4R)-4-({[1-(2,2-Difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic Acid (ABBV/GLPG-2222), a Potent Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Corrector for the Treatment of Cystic Fibrosis.
Wang X, Liu B, Searle X, Yeung C, Bogdan A, Greszler S, Singh A, Fan Y, Swensen AM, Vortherms T, Balut C, Jia Y, Desino K, Gao W, Yong H, Tse C, Kym P. Wang X, et al. Among authors: gao w. J Med Chem. 2018 Feb 22;61(4):1436-1449. doi: 10.1021/acs.jmedchem.7b01339. Epub 2018 Jan 5. J Med Chem. 2018. PMID: 29251932
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach R, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Jia Y, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: gao w. ACS Med Chem Lett. 2019 Oct 31;10(11):1543-1548. doi: 10.1021/acsmedchemlett.9b00377. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749908 Free PMC article.
Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach RJ, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: gao w. Bioorg Med Chem Lett. 2022 Sep 15;72:128843. doi: 10.1016/j.bmcl.2022.128843. Epub 2022 Jun 7. Bioorg Med Chem Lett. 2022. PMID: 35688367
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN. He Y, et al. Among authors: gao w. Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135237
ABT-165, a Dual Variable Domain Immunoglobulin (DVD-Ig) Targeting DLL4 and VEGF, Demonstrates Superior Efficacy and Favorable Safety Profiles in Preclinical Models.
Li Y, Hickson JA, Ambrosi DJ, Haasch DL, Foster-Duke KD, Eaton LJ, DiGiammarino EL, Panchal SC, Jiang F, Mudd SR, Zhang C, Akella SS, Gao W, Ralston SL, Naumovski L, Gu J, Morgan-Lappe SE. Li Y, et al. Among authors: gao w. Mol Cancer Ther. 2018 May;17(5):1039-1050. doi: 10.1158/1535-7163.MCT-17-0800. Epub 2018 Mar 28. Mol Cancer Ther. 2018. PMID: 29592882
The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.
Pappano WN, Guo J, He Y, Ferguson D, Jagadeeswaran S, Osterling DJ, Gao W, Spence JK, Pliushchev M, Sweis RF, Buchanan FG, Michaelides MR, Shoemaker AR, Tse C, Chiang GG. Pappano WN, et al. Among authors: gao w. PLoS One. 2015 Jul 6;10(7):e0131716. doi: 10.1371/journal.pone.0131716. eCollection 2015. PLoS One. 2015. PMID: 26147105 Free PMC article.
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