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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: wang x. 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.
Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.
Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW. Bruncko M, et al. Among authors: wang x. J Med Chem. 2007 Feb 22;50(4):641-62. doi: 10.1021/jm061152t. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256834
Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.
Huth JR, Park C, Petros AM, Kunzer AR, Wendt MD, Wang X, Lynch CL, Mack JC, Swift KM, Judge RA, Chen J, Richardson PL, Jin S, Tahir SK, Matayoshi ED, Dorwin SA, Ladror US, Severin JM, Walter KA, Bartley DM, Fesik SW, Elmore SW, Hajduk PJ. Huth JR, et al. Among authors: wang x. Chem Biol Drug Des. 2007 Jul;70(1):1-12. doi: 10.1111/j.1747-0285.2007.00535.x. Chem Biol Drug Des. 2007. PMID: 17630989
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Petros AM, Huth JR, Oost T, Park CM, Ding H, Wang X, Zhang H, Nimmer P, Mendoza R, Sun C, Mack J, Walter K, Dorwin S, Gramling E, Ladror U, Rosenberg SH, Elmore SW, Fesik SW, Hajduk PJ. Petros AM, et al. Among authors: wang x. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6587-91. doi: 10.1016/j.bmcl.2010.09.033. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20870405
Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.
Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ. Tao ZF, et al. Among authors: wang x, wang l. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25313317 Free PMC article.
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Bruncko M, Wang L, Sheppard GS, Phillips DC, Tahir SK, Xue J, Erickson S, Fidanze S, Fry E, Hasvold L, Jenkins GJ, Jin S, Judge RA, Kovar PJ, Madar D, Nimmer P, Park C, Petros AM, Rosenberg SH, Smith ML, Song X, Sun C, Tao ZF, Wang X, Xiao Y, Zhang H, Tse C, Leverson JD, Elmore SW, Souers AJ. Bruncko M, et al. Among authors: wang x, wang l. J Med Chem. 2015 Mar 12;58(5):2180-94. doi: 10.1021/jm501258m. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25679114
Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.
Bruncko M, Wang L, Sheppard GS, Phillips DC, Tahir SK, Xue J, Erickson S, Fidanze S, Fry E, Hasvold L, Jenkins GJ, Jin S, Judge RA, Kovar PJ, Madar D, Nimmer P, Park C, Petros AM, Rosenberg SH, Smith ML, Song X, Sun C, Tao ZF, Wang X, Xiao Y, Zhang H, Tse C, Leverson JD, Elmore SW, Souers AJ. Bruncko M, et al. Among authors: wang x, wang l. J Med Chem. 2015 May 14;58(9):4089. doi: 10.1021/acs.jmedchem.5b00616. Epub 2015 May 1. J Med Chem. 2015. PMID: 25933255 No abstract available.
Expanding the Repertoire for "Large Small Molecules": Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers.
Salem AH, Tao ZF, Bueno OF, Chen J, Chen S, Edalji R, Elmore SW, Fournier KM, Harper KC, Hong R, Jenkins GJ, Ji J, Judge RA, Kalvass JC, Klix RC, Ku YY, Leverson JD, Marks RA, Marsh KC, Menon RM, Park CH, Phillips DC, Pu YM, Rosenberg SH, Sanzgiri YD, Sheikh AY, Shi Y, Stolarik D, Suleiman AA, Wang X, Zhang GGZ, Catron ND, Souers AJ. Salem AH, et al. Among authors: wang x. Mol Cancer Ther. 2021 Jun;20(6):999-1008. doi: 10.1158/1535-7163.MCT-21-0077. Epub 2021 Mar 30. Mol Cancer Ther. 2021. PMID: 33785651
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