Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour act... von Wilson, Wyndham H, Prof, O'Connor, Owen A, Prof, Czuczman, Myron S, Prof, LaCasce, Ann S, MD, Gerecitano, John F, MD, Leonard, John P, Prof, Tulpule, Anil, MD, Dunleavy, Kieron, MD, Xiong, Hao, PhD, Chiu, Yi-Lin, PhD, Cui, Yue, PhD, Busman, Todd, MS, Elmore, Steven W, PhD, Rosenberg, Saul H, PhD, Krivoshik, Andrew P, MD, Enschede, Sari H, MD, Humerickhouse, Rod A, MD

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ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor von Tse, Christin, Shoemaker, Alexander R, Adickes, Jessica, Anderson, Mark G, Chen, Jun, Jin, Sha, Johnson, Eric F, Marsh, Kennan C, Mitten, Michael J, Nimmer, Paul, Roberts, Lisa, Tahir, Stephen K, Xiao, Yu, Yang, Xiufen, Zhang, Haichao, Fesik, Stephen, Rosenberg, Saul H, Elmore, Steven W

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MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor von Xiao, Yu, Nimmer, Paul, Sheppard, George S, Bruncko, Milan, Hessler, Paul, Lu, Xin, Roberts-Rapp, Lisa, Pappano, William N, Elmore, Steven W, Souers, Andrew J, Leverson, Joel D, Phillips, Darren C

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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 Br... von McDaniel, Keith F, Wang, Le, Soltwedel, Todd, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Mantei, Robert A, Pratt, John K, Sheppard, George S, Bui, Mai H, Faivre, Emily J, Huang, Xiaoli, Li, Leiming, Lin, Xiaoyu, Wang, Rongqi, Warder, Scott E, Wilcox, Denise, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Park, Chang H, Hutchins, Charles W, Shen, Jianwei J, Edalji, Rohinton P, Sun, Chaohong C, Martin, Ruth, Gao, Wenqing, Wong, Shekman, Fang, Guowei, Elmore, Steven W, Shen, Yu, Kati, Warren M

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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies von 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 an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins von Park, Cheol-Min, Bruncko, Milan, Adickes, Jessica, Bauch, Joy, Ding, Hong, Kunzer, Aaron, Marsh, Kennan C, Nimmer, Paul, Shoemaker, Alexander R, Song, Xiaohong, Tahir, Stephen K, Tse, Christin, Wang, Xilu, Wendt, Michael D, Yang, Xiufen, Zhang, Haichao, Fesik, Stephen W, Rosenberg, Saul H, Elmore, Steven W

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Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models von SHOEMAKER, Alex R, MITTEN, Michael J, BAUCH, Joy, MARSH, Kennan, TAHIR, Steven K, XIUFENYANG, TSE, Christin, FESIK, Stephen W, ROSENBERG, Saul H, ELMORE, Steven W, ADICKES, Jessica, ACKLER, Scott, REFICI, Marion, FERGUSON, Debra, OLEKSIJEW, Anatol, O'CONNOR, Jacqueline M, BAOLE WANG, FROST, David J

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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity von 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 von 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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ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets von Souers, Andrew J, Leverson, Joel D, Boghaert, Erwin R, Ackler, Scott L, Catron, Nathaniel D, Chen, Jun, Dayton, Brian D, Ding, Hong, Enschede, Sari H, Fairbrother, Wayne J, Huang, David C S, Hymowitz, Sarah G, Jin, Sha, Khaw, Seong Lin, Kovar, Peter J, Lam, Lloyd T, Lee, Jackie, Maecker, Heather L, Marsh, Kennan C, Mason, Kylie D, Mitten, Michael J, Nimmer, Paul M, Oleksijew, Anatol, Park, Chang H, Park, Cheol-Min, Phillips, Darren C, Roberts, Andrew W, Sampath, Deepak, Seymour, John F, Smith, Morey L, Sullivan, Gerard M, Tahir, Stephen K, Tse, Chris, Wendt, Michael D, Xiao, Yu, Xue, John C, Zhang, Haichao, Humerickhouse, Rod A, Rosenberg, Saul H, Elmore, Steven W

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Discovery of a Potent and Selective BCL‑XL Inhibitor with in Vivo Activity von 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

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An inhibitor of Bcl-2 family proteins induces regression of solid tumours von Fesik, Stephen W, Rosenberg, Saul H, Oltersdorf, Tilman, Elmore, Steven W, Shoemaker, Alexander R, Armstrong, Robert C, Augeri, David J, Belli, Barbara A, Bruncko, Milan, Deckwerth, Thomas L, Dinges, Jurgen, Hajduk, Philip J, Joseph, Mary K, Kitada, Shinichi, Korsmeyer, Stanley J, Kunzer, Aaron R, Letai, Anthony, Li, Chi, Mitten, Michael J, Nettesheim, David G, Ng, ShiChung, Nimmer, Paul M, O'Connor, Jacqueline M, Oleksijew, Anatol, Petros, Andrew M, Reed, John C, Shen, Wang, Tahir, Stephen K, Thompson, Craig B, Tomaselli, Kevin J, Wang, Baole, Wendt, Michael D, Zhang, Haichao

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The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo von Ackler, Scott, Mitten, Michael J., Foster, Kelly, Oleksijew, Anatol, Refici, Marion, Tahir, Stephen K., Xiao, Yu, Tse, Christin, Frost, David J., Fesik, Stephen W., Rosenberg, Saul H., Elmore, Steven W., Shoemaker, Alexander R.

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Role of mitochondrial inner membrane permeabilization in necrotic cell death, apoptosis, and autophagy von Lemasters, John J, Qian, Ting, He, Lihua, Kim, Jae-Sung, Elmore, Steven P, Cascio, Wayne E, Brenner, David A

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Discovery of Potent Antagonists of the Antiapoptotic Protein XIAP for the Treatment of Cancer von Oost, Thorsten K, Sun, Chaohong, Armstrong, Robert C, Al-Assaad, Ali-Samer, Betz, Stephen F, Deckwerth, Thomas L, Ding, Hong, Elmore, Steven W, Meadows, Robert P, Olejniczak, Edward T, Oleksijew, Andrew, Oltersdorf, Tilman, Rosenberg, Saul H, Shoemaker, Alexander R, Tomaselli, Kevin J, Zou, Hua, Fesik, Stephen W

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Expanding the Repertoire for "Large Small Molecules": Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers von Salem, Ahmed Hamed, Tao, Zhi-Fu, Bueno, Orlando F., Chen, Jie, Chen, Shuang, Edalji, Rohinton, Elmore, Steven W., Fournier, Keith M., Harper, Kaid C., Hong, Richard, Jenkins, Gary J., Ji, Jianguo, Judge, Russell A., Kalvass, John C., Klix, Russell C., Ku, Yi-Yin, Leverson, Joel D., Marks, Richard A., Marsh, Kennan C., Menon, Rajeev M., Park, Chang H., Phillips, Darren C., Pu, Yu-Ming, Rosenberg, Saul H., Sanzgiri, Yeshwant D., Sheikh, Ahmad Y., Shi, Yi, Stolarik, Deanne, Suleiman, Ahmed A., Wang, Xilu, Zhang, Geoff G. Z., Catron, Nathaniel D., Souers, Andrew J.

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Structure-Based Design of A-1293102, a Potent and Selective BCL-X-L Inhibitor von Tao, Zhi-Fu, Wang, Xilu, Chen, Jun, Ingram, Justin P., Jin, Sha, Judge, Russell A., Kovar, Peter J., Park, Chang, Sun, Chaohong, Wakefield, Brian D., Zhou, Li, Zhang, Haichao, Elmore, Steven W., Phillips, Darren C., Judd, Andrew S., Leverson, Joel D., Souers, Andrew J.

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Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR von Petros, Andrew M., Huth, Jeffrey R., Oost, Thorsten, Park, Cheol-Min, Ding, Hong, Wang, Xilu, Zhang, Haichao, Nimmer, Paul, Mendoza, Renaldo, Sun, Chaohong, Mack, Jamey, Walter, Karl, Dorwin, Sarah, Gramling, Emily, Ladror, Uri, Rosenberg, Saul H., Elmore, Steven W., Fesik, Stephen W., Hajduk, Philip J.

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Methylpyrrole inhibitors of BET bromodomains von Hasvold, Lisa A., Sheppard, George S., Wang, Le, Fidanze, Steven D., Liu, Dachun, Pratt, John K., Mantei, Robert A., Wada, Carol K., Hubbard, Robbert, Shen, Yu, Lin, Xiaoyu, Huang, Xiaoli, Warder, Scott E., Wilcox, Denise, Li, Leiming, Buchanan, F. Greg, Smithee, Lauren, Albert, Daniel H., Magoc, Terrance J., Park, Chang H., Petros, Andrew M., Panchal, Sanjay C., Sun, Chaohong, Kovar, Peter, Soni, Nirupama B., Elmore, Steven W., Kati, Warren M., McDaniel, Keith F.

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The mitochondrial permeability transition initiates autophagy in rat hepatocytes von Elmore, Steven P., Qian, Ting, Grissom, Sherry F., Lemasters, John J.

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