Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy
Leverson, Joel D, Phillips, Darren C, Mitten, Michael J, Boghaert, Erwin R, Diaz, Dolores, Tahir, Stephen K, Belmont, Lisa D, Nimmer, Paul, Xiao, Yu, Ma, Xiaoju Max, Lowes, Kym N, Kovar, Peter, Chen, Jun, Jin, Sha, Smith, Morey, Xue, John, Zhang, Haichao, Oleksijew, Anatol, Magoc, Terrance J, Vaidya, Kedar S, Albert, Daniel H, Tarrant, Jacqueline M, La, Nghi, Wang, Le, Tao, Zhi-Fu, Wendt, Michael D, Sampath, Deepak, Rosenberg, Saul H, Tse, Chris, Huang, David C S, Fairbrother, Wayne J, Elmore, Steven W, Souers, Andrew J
Published in Science translational medicine (18.03.2015)
Published in Science translational medicine (18.03.2015)
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ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor
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
Published in Cancer research (Chicago, Ill.) (01.05.2008)
Published in Cancer research (Chicago, Ill.) (01.05.2008)
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Journal Article
MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor
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
Published in Molecular cancer therapeutics (01.08.2015)
Published in Molecular cancer therapeutics (01.08.2015)
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Journal Article
Discovery of an Orally Bioavailable Small Molecule Inhibitor of Prosurvival B-Cell Lymphoma 2 Proteins
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
Published in Journal of medicinal chemistry (13.11.2008)
Published in Journal of medicinal chemistry (13.11.2008)
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Journal Article
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets
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
Published in Nature medicine (01.02.2013)
Published in Nature medicine (01.02.2013)
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Journal Article
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR
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.
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
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Discovery and Structure−Activity Relationship of Antagonists of B-Cell Lymphoma 2 Family Proteins with Chemopotentiation Activity in Vitro and in Vivo
Wendt, Michael D, Shen, Wang, Kunzer, Aaron, McClellan, William J, Bruncko, Milan, Oost, Thorsten K, Ding, Hong, Joseph, Mary K, Zhang, Haichao, Nimmer, Paul M, Ng, Shi-Chung, Shoemaker, Alexander R, Petros, Andrew M, Oleksijew, Anatol, Marsh, Kennan, Bauch, Joy, Oltersdorf, Tilman, Belli, Barbara A, Martineau, Darlene, Fesik, Stephen W, Rosenberg, Saul H, Elmore, Steven W
Published in Journal of medicinal chemistry (09.02.2006)
Published in Journal of medicinal chemistry (09.02.2006)
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Journal Article
Studies Leading to Potent, Dual Inhibitors of Bcl-2 and Bcl-xL
Bruncko, Milan, Oost, Thorsten K, Belli, Barbara A, Ding, Hong, Joseph, Mary K, Kunzer, Aaron, Martineau, Darlene, McClellan, William J, Mitten, Michael, Ng, Shi-Chung, Nimmer, Paul M, Oltersdorf, Tilman, Park, Cheol-Min, Petros, Andrew M, Shoemaker, Alexander R, Song, Xiaohong, Wang, Xilu, Wendt, Michael D, Zhang, Haichao, Fesik, Stephen W, Rosenberg, Saul H, Elmore, Steven W
Published in Journal of medicinal chemistry (22.02.2007)
Published in Journal of medicinal chemistry (22.02.2007)
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Journal Article
Development of a high-throughput fluorescence polarization assay for Bcl-xL
Zhang, Haichao, Nimmer, Paul, Rosenberg, Saul H, Ng, Shi-Chung, Joseph, Mary
Published in Analytical biochemistry (01.08.2002)
Published in Analytical biochemistry (01.08.2002)
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Journal Article
The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo
Chen, Jun, Jin, Sha, Abraham, Vivek, Huang, Xiaoli, Liu, Bernard, Mitten, Michael J., Nimmer, Paul, Lin, Xiaoyu, Smith, Morey, Shen, Yu, Shoemaker, Alexander R., Tahir, Stephen K., Zhang, Haichao, Ackler, Scott L., Rosenberg, Saul H., Maecker, Heather, Sampath, Deepak, Leverson, Joel D., Tse, Chris, Elmore, Steven W.
Published in Molecular cancer therapeutics (01.12.2011)
Published in Molecular cancer therapeutics (01.12.2011)
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Journal Article
Design, Synthesis, and Computational Studies of Inhibitors of Bcl-XL
Park, Cheol-Min, Oie, Tetsuro, Petros, Andrew M, Zhang, Haichao, Nimmer, Paul M, Henry, Rodger F, Elmore, Steven W
Published in Journal of the American Chemical Society (20.12.2006)
Published in Journal of the American Chemical Society (20.12.2006)
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Journal Article
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
Published in Journal of medicinal chemistry (12.03.2015)
Published in Journal of medicinal chemistry (12.03.2015)
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Journal Article
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X-L Inhibitor
Wang, Le, Doherty, George A., Judd, Andrew S., Tao, Zhi-Fu, Hansen, T. Matthew, Frey, Robin R., Song, Xiaohong, Bruncko, Milan, Kunzer, Aaron R., Wang, Xilu, Wendt, Michael D., Flygare, John A., Catron, Nathaniel D., Judge, Russell A., Park, Chang H., Shekhar, Shashank, Phillips, Darren C., Nimmer, Paul, Smith, Morey L., Tahir, Stephen K., Xiao, Yu, Xue, John, Zhang, Haichao, Le, Phuong N., Mitten, Michael J., Boghaert, Erwin R., Gao, Wenqing, Kovar, Peter, Choo, Edna F., Diaz, Dolores, Fairbrother, Wayne J., Elmore, Steven W., Sampath, Deepak, Leverson, Joel D., Souers, Andrew James
Published in ACS medicinal chemistry letters (08.10.2020)
Published in ACS medicinal chemistry letters (08.10.2020)
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Journal Article
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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Journal Article
An inhibitor of Bcl-2 family proteins induces regression of solid tumours
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
Published in Nature (02.06.2005)
Published in Nature (02.06.2005)
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Journal Article
A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo
SHOEMAKER, Alex R, OLEKSIJEW, Anatol, MARSH, Kennan, MCCLELLAN, William, NELLANS, Hugh, NG, Shichung, NIMMER, Paul, O'CONNOR, Jacqueline M, OLTERSDORF, Tilman, WEIGUO QING, WANG SHEN, STAVROPOULOS, Jason, BAUCH, Joy, TAHIR, Stephen K, BAOLE WANG, WARNER, Robert, HAICHAO ZHANG, FESIK, Stephen W, ROSENBERG, Saul H, ELMORE, Steven W, BELLI, Barbara A, BORRE, Tony, BRUNCKO, Milan, DECKWIRTH, Thomas, FROST, David J, JARVIS, Ken, JOSEPH, Mary K
Published in Cancer research (Chicago, Ill.) (01.09.2006)
Published in Cancer research (Chicago, Ill.) (01.09.2006)
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Glycan-Mediated, Ligand-Controlled Click Chemistry for Drug-Target Identification
Stöckmann, Henning, Marin, Violeta L., Nimmer, Paul, Balut, Corina M., Davidson, Donald J., Richardson, Paul L., Vasudevan, Anil
Published in Chembiochem : a European journal of chemical biology (15.01.2016)
Published in Chembiochem : a European journal of chemical biology (15.01.2016)
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Journal Article
BCL-XL-targeting antibody-drug conjugates are active in preclinical models and mitigate on-mechanism toxicity of small-molecule inhibitors
Judd, Andrew S, Bawa, Bhupinder, Buck, Wayne R, Tao, Zhi-Fu, Li, Yingchun, Mitten, Michael J, Bruncko, Milan, Catron, Nathaniel, Doherty, George, Durbin, Kenneth R, Enright, Brian, Frey, Robin, Haasch, Deanna, Haman, Sandra, Haight, Anthony R, Henriques, Tracy A, Holms, James, Izeradjene, Kamel, Judge, Russell A, Jenkins, Gary J, Kunzer, Aaron, Leverson, Joel D, Martin, Ruth L, Mitra, Diya, Mittelstadt, Scott, Nelson, Lorne, Nimmer, Paul, Palma, Joann, Peterson, Richard, Phillips, Darren C, Ralston, Sherry L, Rosenberg, Saul H, Shen, Xiaoqiang, Song, Xiaohong, Vaidya, Kedar R, Wang, Xilu, Wang, Jin, Xiao, Yu, Zhang, Haichao, Zhang, Xinxin, Blomme, Eric A, Boghaert, Erwin R, Kalvass, John C, Phillips, Andrew, Souers, Andrew J
Published in Science advances (04.10.2024)
Published in Science advances (04.10.2024)
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Journal Article
BCL-X L -targeting antibody-drug conjugates are active in preclinical models and mitigate on-mechanism toxicity of small-molecule inhibitors
Judd, Andrew S, Bawa, Bhupinder, Buck, Wayne R, Tao, Zhi-Fu, Li, Yingchun, Mitten, Michael J, Bruncko, Milan, Catron, Nathaniel, Doherty, George, Durbin, Kenneth R, Enright, Brian, Frey, Robin, Haasch, Deanna, Haman, Sandra, Haight, Anthony R, Henriques, Tracy A, Holms, James, Izeradjene, Kamel, Judge, Russell A, Jenkins, Gary J, Kunzer, Aaron, Leverson, Joel D, Martin, Ruth L, Mitra, Diya, Mittelstadt, Scott, Nelson, Lorne, Nimmer, Paul, Palma, Joann, Peterson, Richard, Phillips, Darren C, Ralston, Sherry L, Rosenberg, Saul H, Shen, Xiaoqiang, Song, Xiaohong, Vaidya, Kedar R, Wang, Xilu, Wang, Jin, Xiao, Yu, Zhang, Haichao, Zhang, Xinxin, Blomme, Eric A, Boghaert, Erwin R, Kalvass, John C, Phillips, Andrew, Souers, Andrew J
Published in Science advances (04.10.2024)
Published in Science advances (04.10.2024)
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Journal Article
Discovery of A‑1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL‑XL Inhibitor
Wang, Le, Doherty, George A, Judd, Andrew S, Tao, Zhi-Fu, Hansen, T. Matthew, Frey, Robin R, Song, Xiaohong, Bruncko, Milan, Kunzer, Aaron R, Wang, Xilu, Wendt, Michael D, Flygare, John A, Catron, Nathaniel D, Judge, Russell A, Park, Chang H, Shekhar, Shashank, Phillips, Darren C, Nimmer, Paul, Smith, Morey L, Tahir, Stephen K, Xiao, Yu, Xue, John, Zhang, Haichao, Le, Phuong N, Mitten, Michael J, Boghaert, Erwin R, Gao, Wenqing, Kovar, Peter, Choo, Edna F, Diaz, Dolores, Fairbrother, Wayne J, Elmore, Steven W, Sampath, Deepak, Leverson, Joel D, Souers, Andrew James
Published in ACS medicinal chemistry letters (08.10.2020)
Published in ACS medicinal chemistry letters (08.10.2020)
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