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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: souers aj. J Med Chem. 2015 Mar 12;58(5):2180-94. doi: 10.1021/jm501258m. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25679114
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: souers aj. 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.
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: souers aj. 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.
Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor.
Tao ZF, Wang X, Chen J, Ingram JP, Jin S, Judge RA, Kovar PJ, Park C, Sun C, Wakefield BD, Zhou L, Zhang H, Elmore SW, Phillips DC, Judd AS, Leverson JD, Souers AJ. Tao ZF, et al. Among authors: souers aj. ACS Med Chem Lett. 2021 May 12;12(6):1011-1016. doi: 10.1021/acsmedchemlett.1c00162. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141086 Free PMC article.
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.
Tong Y, Florjancic AS, Clark RF, Lai C, Mastracchio A, Zhu GD, Smith ML, Kovar PJ, Shaw B, Albert DH, Qiu W, Longenecker KL, Liu X, Olson AM, Osterling DJ, Tahir SK, Phillips DC, Leverson JD, Souers AJ, Penning TD. Tong Y, et al. Among authors: souers aj. ACS Med Chem Lett. 2021 Jun 22;12(7):1108-1115. doi: 10.1021/acsmedchemlett.1c00161. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267880 Free PMC article.
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: souers aj. 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.
Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
Leverson JD, Zhang H, Chen J, Tahir SK, Phillips DC, Xue J, Nimmer P, Jin S, Smith M, Xiao Y, Kovar P, Tanaka A, Bruncko M, Sheppard GS, Wang L, Gierke S, Kategaya L, Anderson DJ, Wong C, Eastham-Anderson J, Ludlam MJ, Sampath D, Fairbrother WJ, Wertz I, Rosenberg SH, Tse C, Elmore SW, Souers AJ. Leverson JD, et al. Among authors: souers aj. Cell Death Dis. 2015 Jan 15;6(1):e1590. doi: 10.1038/cddis.2014.561. Cell Death Dis. 2015. PMID: 25590800 Free PMC article.
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW. Souers AJ, et al. Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6. Nat Med. 2013. PMID: 23291630
76 results