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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: chen j. 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 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: chen j. 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.
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: chen j. 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: chen j. Sci Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642. Sci Transl Med. 2015. PMID: 25787766
A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies.
Phillips DC, Jin S, Gregory GP, Zhang Q, Xue J, Zhao X, Chen J, Tong Y, Zhang H, Smith M, Tahir SK, Clark RF, Penning TD, Devlin JR, Shortt J, Hsi ED, Albert DH, Konopleva M, Johnstone RW, Leverson JD, Souers AJ. Phillips DC, et al. Among authors: chen j. Leukemia. 2020 Jun;34(6):1646-1657. doi: 10.1038/s41375-019-0652-0. Epub 2019 Dec 11. Leukemia. 2020. PMID: 31827241 Free PMC article.
N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.
Bruncko M, Tahir SK, Song X, Chen J, Ding H, Huth JR, Jin S, Judge RA, Madar DJ, Park CH, Park CM, Petros AM, Tse C, Rosenberg SH, Elmore SW. Bruncko M, et al. Among authors: chen j. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7503-6. doi: 10.1016/j.bmcl.2010.10.010. Epub 2010 Oct 12. Bioorg Med Chem Lett. 2010. PMID: 21106457
Clearance of systemic hematologic tumors by venetoclax (Abt-199) and navitoclax.
Ackler S, Oleksijew A, Chen J, Chyla BJ, Clarin J, Foster K, McGonigal T, Mishra S, Schlessinger S, Smith ML, Tahir SK, Leverson JD, Souers AJ, Boghaert ER, Hickson J. Ackler S, et al. Among authors: chen j. Pharmacol Res Perspect. 2015 Oct;3(5):e00178. doi: 10.1002/prp2.178. Epub 2015 Sep 1. Pharmacol Res Perspect. 2015. PMID: 26516589 Free PMC article.
The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo.
Chen J, Jin S, Abraham V, Huang X, Liu B, Mitten MJ, Nimmer P, Lin X, Smith M, Shen Y, Shoemaker AR, Tahir SK, Zhang H, Ackler SL, Rosenberg SH, Maecker H, Sampath D, Leverson JD, Tse C, Elmore SW. Chen J, et al. Mol Cancer Ther. 2011 Dec;10(12):2340-9. doi: 10.1158/1535-7163.MCT-11-0415. Epub 2011 Sep 13. Mol Cancer Ther. 2011. PMID: 21914853
Discovery of a novel small molecule binding site of human survivin.
Wendt MD, Sun C, Kunzer A, Sauer D, Sarris K, Hoff E, Yu L, Nettesheim DG, Chen J, Jin S, Comess KM, Fan Y, Anderson SN, Isaac B, Olejniczak ET, Hajduk PJ, Rosenberg SH, Elmore SW. Wendt MD, et al. Among authors: chen j. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3122-9. doi: 10.1016/j.bmcl.2007.03.042. Epub 2007 Mar 16. Bioorg Med Chem Lett. 2007. PMID: 17391963
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