Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity
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Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins
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Published in Journal of medicinal chemistry (13.11.2008)
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Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models
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The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo
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Discovery of Potent Antagonists of the Antiapoptotic Protein XIAP for the Treatment of Cancer
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Published in Journal of medicinal chemistry (26.08.2004)
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Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
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Published in Bioorganic & medicinal chemistry letters (15.11.2010)
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ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo
Ackler, Scott, Xiao, Yu, Mitten, Michael J, Foster, Kelly, Oleksijew, Anatol, Refici, Marion, Schlessinger, Sally, Wang, Baole, Chemburkar, Sanjay R, Bauch, Joy, Tse, Christin, Frost, David J, Fesik, Stephen W, Rosenberg, Saul H, Elmore, Steven W, Shoemaker, Alex R
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Published in Bioorganic & medicinal chemistry letters (01.06.2007)
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Published in Nature medicine (01.02.2013)
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Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy
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Nonsteroidal Selective Glucocorticoid Modulators: The Effect of C-10 Substitution on Receptor Selectivity and Functional Potency of 5-Allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines
Kym, Philip R, Kort, Michael E, Coghlan, Michael J, Moore, Jimmie L, Tang, Rui, Ratajczyk, James D, Larson, Daniel P, Elmore, Steven W, Pratt, John K, Stashko, Michael A, Falls, H. Douglass, Lin, Chun W, Nakane, Masake, Miller, Loan, Tyree, Curtis M, Miner, Jeffery N, Jacobson, Peer B, Wilcox, Denise M, Nguyen, Phong, Lane, Benjamin C
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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies
Bui, Mai H, Lin, Xiaoyu, Albert, Daniel H, Li, Leiming, Lam, Lloyd T, Faivre, Emily J, Warder, Scott E, Huang, Xiaoli, Wilcox, Denise, Donawho, Cherrie K, Sheppard, George S, Wang, Le, Fidanze, Steve, Pratt, John K, Liu, Dachun, Hasvold, Lisa, Uziel, Tamar, Lu, Xin, Kohlhapp, Fred, Fang, Guowei, Elmore, Steven W, Rosenberg, Saul H, McDaniel, Keith F, Kati, Warren M, Shen, Yu
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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
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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity
Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors
Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F
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Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity
Tao, Zhi-Fu, Hasvold, Lisa, Wang, Le, Wang, Xilu, Petros, Andrew M, Park, Chang H, Boghaert, Erwin R, Catron, Nathaniel D, Chen, Jun, Colman, Peter M, Czabotar, Peter E, Deshayes, Kurt, Fairbrother, Wayne J, Flygare, John A, Hymowitz, Sarah G, Jin, Sha, Judge, Russell A, Koehler, Michael F. T, Kovar, Peter J, Lessene, Guillaume, Mitten, Michael J, Ndubaku, Chudi O, Nimmer, Paul, Purkey, Hans E, Oleksijew, Anatol, Phillips, Darren C, Sleebs, Brad E, Smith, Brian J, Smith, Morey L, Tahir, Stephen K, Watson, Keith G, Xiao, Yu, Xue, John, Zhang, Haichao, Zobel, Kerry, Rosenberg, Saul H, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
Published in ACS medicinal chemistry letters (09.10.2014)
Published in ACS medicinal chemistry letters (09.10.2014)
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An inhibitor of Bcl-2 family proteins induces regression of solid tumours
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Published in Nature (02.06.2005)
Published in Nature (02.06.2005)
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Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators
Elmore, Steven W, Pratt, John K, Coghlan, Michael J, Mao, Yue, Green, Brian E, Anderson, David D, Stashko, Michael A, Lin, Chun W, Falls, Douglas, Nakane, Masaki, Miller, Loan, Tyree, Curtis M, Miner, Jeffrey N, Lane, Ben
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
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