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Page 1
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: elmore sw. 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
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. Among authors: elmore sw. Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6. Nat Med. 2013. PMID: 23291630
Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.
Leverson JD, Phillips DC, Mitten MJ, Boghaert ER, Diaz D, Tahir SK, Belmont LD, Nimmer P, Xiao Y, Ma XM, Lowes KN, Kovar P, Chen J, Jin S, Smith M, Xue J, Zhang H, Oleksijew A, Magoc TJ, Vaidya KS, Albert DH, Tarrant JM, La N, Wang L, Tao ZF, Wendt MD, Sampath D, Rosenberg SH, Tse C, Huang DC, Fairbrother WJ, Elmore SW, Souers AJ. Leverson JD, et al. Among authors: elmore sw. Sci Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642. Sci Transl Med. 2015. PMID: 25787766
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: elmore sw. J Med Chem. 2015 Mar 12;58(5):2180-94. doi: 10.1021/jm501258m. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25679114
Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.
Bui MH, Lin X, Albert DH, Li L, Lam LT, Faivre EJ, Warder SE, Huang X, Wilcox D, Donawho CK, Sheppard GS, Wang L, Fidanze S, Pratt JK, Liu D, Hasvold L, Uziel T, Lu X, Kohlhapp F, Fang G, Elmore SW, Rosenberg SH, McDaniel KF, Kati WM, Shen Y. Bui MH, et al. Among authors: elmore sw. Cancer Res. 2017 Jun 1;77(11):2976-2989. doi: 10.1158/0008-5472.CAN-16-1793. Epub 2017 Apr 17. Cancer Res. 2017. PMID: 28416490
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: elmore sw. 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.
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: elmore sw. 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.
Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines.
Tahir SK, Wass J, Joseph MK, Devanarayan V, Hessler P, Zhang H, Elmore SW, Kroeger PE, Tse C, Rosenberg SH, Anderson MG. Tahir SK, et al. Among authors: elmore sw. Mol Cancer Ther. 2010 Mar;9(3):545-57. doi: 10.1158/1535-7163.MCT-09-0651. Epub 2010 Feb 23. Mol Cancer Ther. 2010. PMID: 20179162
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: elmore sw. Cell Death Dis. 2015 Jan 15;6(1):e1590. doi: 10.1038/cddis.2014.561. Cell Death Dis. 2015. PMID: 25590800 Free PMC article.
50 results