未登录 Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo Randolph, John T.; O'Connor, Matthew J.; Han, Fei; Hutchins, Charles W.; Siu, Y. Amy; Cho, Min; Zheng, Yunan; Hickson, Jonathan A.; Markley, Jana L.; Manaves, Vlasios; Algire, Mikkel; Baker, Kenton A.; Chapman, Alex M.; Gopalakrishnan, Sujatha M.; Panchal, Sanjay C.; Foster-Duke, Kelly; Stolarik, DeAnne F.; Kempf-Grote, Anita; Dammeier, Darby; Fossey, Stacey; Sun, Qi; Sun, Chaohong; Shen, Yu; Dart, Michael J.; Kati, Warren M.; Lai, Albert; Firestone, Ari J.; Kort, Michael E. 分享 收藏
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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia Zhang, Lu; Cai, Tianyu; Lin, Xiaoyu; Huang, Xiaoli; Bui, Mai H.; Plotnik, Joshua P.; Bellin, Richard J.; Faivre, Emily J.; Kuruvilla, Vinitha M.; Lam, Lloyd T.; Lu, Xin; Zha, Zheng; Feng, Weiguo; Hessler, Paul; Uziel, Tamar; Zhang, Qi; Cavazos, Antonio; Han, Lina; Ferguson, Debra C.; Mehta, Gaurav; Shanmugavelandy, Sriram S.; Magoc, Terrance J.; Rowe, Jenny; Goodwin, Neal C.; Dorritie, Kathleen A.; Boyiadzis, Michael; Albert, Daniel H.; McDaniel, Keith F.; Kati, Warren M.; Konopleva, Marina; Shen, Yu 分享 收藏
Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Pratt, John K.; Park, Chang H.; Longenecker, Kenton; Qiu, Wei; Torrent, Maricel; Kovar, Peter J.; Bui, Mai; Faivre, Emily; Huang, Xiaoli; Lin, Xiaoyu; Wilcox, Denise; Zhang, Lu; Shen, Yu; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Kati, Warren M.; McDaniel, Keith F. 分享 收藏
Acute myeloid leukemia human/mouse co-clinical trial feasibility study optimized in human transgenic IL-3/GMCSF NOD/Shi-scid-IL2rnull mice Goodwin, Neal C.; Albert, Daniel H.; Davies, Angela M.; Rowe, Jenny; Feuer, Gerold; Boyiadzis, Michael; Dorritie, Kathleen A.; Mancini, Maria; Gandour-Edwards, Regina; Kati, Warren M.; McKee, Mark D.; McDaniel, Keith F.; Frost, David J. 分享 收藏
First-in-class, highly BDII-selective BET family inhibitor ABBV-744 displays potent anti-tumor activity in androgen receptor positive prostate cancer models and an improved tolerability profile Faivre, Emily J.; Wilcox, Denise; Mai Ha-Bui; Hessler, Paul; Sehgal, Vasudha; Lu, Xin; Uziel, Tamar; Mehta, Gaurav; Albert, Daniel H.; McDaniel, Keith; Kati, Warren; Shen, Yu 分享 收藏
Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor Sheppard, George S.; Wang, Le; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Pratt, John K.; Park, Chang H.; Bui, Mai-Ha; Faivre, Emily J.; Huang, Xiaoli; Lin, Xiaoyu; Wilcox, Denise M.; Shen, Yu; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Kati, Warren M.; McDaniel, Keith F. 分享 收藏
Highlights of the Structure-Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530) Wagner, Rolf; Randolph, John T.; Patel, Sachin V.; Nelson, Lissa; Matulenko, Mark A.; Keddy, Ryan; Pratt, John K.; Liu, Dachun; Krueger, A. Chris; Donner, Pamela L.; Hutchinson, Douglas K.; Flentge, Charles; Betebenner, David; Rockway, Todd; Maring, Clarence J.; Ng, Teresa I.; Krishnan, Preethi; Pilot-Matias, Tami; Collins, Christine; Panchal, Neeta; Reisch, Thomas; Dekhtyar, Tatyana; Mondal, Rubina; Stolarik, DeAnne F.; Gao, Yi; Gao, Wenqing; Beno, David A.; Kati, Warren M. 分享 收藏
Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability Randolph, John T.; Krueger, A. Chris; Donner, Pamela L.; Pratt, John K.; Liu, Dachun; Motter, Christopher E.; Rockway, Todd W.; Tufano, Michael D.; Wagner, Rolf; Lim, Hock B.; Beyer, Jill M.; Mondal, Rubina; Panchal, Neeta S.; Colletti, Lynn; Liu, Yaya; Koev, Gennadiy; Kati, Warren M.; Hernandez, Lisa E.; Beno, David W. A.; Longenecker, Kenton L.; Stewart, Kent D.; Dumas, Emily O.; Molla, Akhteruzzaman; Maring, Clarence J. 分享 收藏
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 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. 分享 收藏
Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors Lam, Lloyd T.; Lin, Xiaoyu; Faivre, Emily J.; Yang, Ziping; Huang, Xiaoli; Wilcox, Denise M.; Bellin, Richard J.; Jin, Sha; Tahir, Stephen K.; Mitten, Michael; Magoc, Terry; Bhathena, Anahita; Kati, Warren M.; Albert, Daniel H.; Shen, Yu; Uziel, Tamar 分享 收藏
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 分享 收藏
In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS5A Inhibitor Pibrentasvir Ng, Teresa I.; Krishnan, Preethi; Pilot-Matias, Tami; Kati, Warren; Schnell, Gretja; Beyer, Jill; Reisch, Thomas; Lu, Liangjun; Dekhtyar, Tatyana; Irvin, Michelle; Tripathi, Rakesh; Maring, Clarence; Randolph, John T.; Wagner, Rolf; Collins, Christine 分享 收藏
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. 分享 收藏
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Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075 Faivre, Emily J.; Wilcox, Denise; Lin, Xiaoyu; Hessler, Paul; Torrent, Maricel; He, Wei; Uziel, Tamar; Albert, Daniel H.; McDaniel, Keith; Kati, Warren; Shen, Yu 分享 收藏
HEXIM1 as a pharmacodynamic marker for monitoring target engagement of ABBV-075 Huang, Xiaoli; Lin, Xiaoyu; Li, Leiming; Wang, Rongqi; Roberts, Lisa; Hessler, Paul; Uziel, Tamar; Lam, Lloyd; Magoc, Terry; Albert, Daniel H.; Elmore, Steven W.; Fang, Guowei; Rosenberg, Saul H.; McDaniel, Keith; Kati, Warren; Shen, Yu 分享 收藏
Potent inhibition of bromodomain-containing BET family with ABBV-075 induces robust antitumor efficacy in preclinical models of breast cancer and exhibits in vitro synergy with doxorubicin Faivre, Emily J.; Lin, Xiaoyu; Wilcox, Denise M.; Huang, Xiaoli; Sarthy, Aparna; Magoc, Terry; Albert, Daniel H.; Fang, Guowei; Rosenberg, Saul H.; McDaniel, Keith F.; Kati, Warren M.; Shen, Yu 分享 收藏
ABBV-075, a novel BET family bromodomain inhibitor, represents a promising therapeutic agent for a broad spectrum of cancer indications Sarthy, Aparna; Li, Leiming; Albert, Daniel H.; Lin, Xiaoyu; Scott, Warder; Faivre, Emily; Bui, Mai H.; Huang, Xiaoli; Wilcox, Denise M.; Magoc, Terry; Buchanan, Fritz G.; Tapang, Paul; Sheppard, George S.; Le Wang; Fidanze, Steve D.; Pratt, John; Liu, Dachun; Hasvold, Lisa; Hessler, Paul; Uziel, Tamar; Lam, Lloyd; Rajaraman, Ganesh; Fang, Guowei; Elmore, Steven W.; Rosenberg, Saul H.; McDaniel, Keith; Kati, Warren; Shen, Yu 分享 收藏
Functional group elaboration of a low molecular weight fragment to yield the novel BET family bromodomain inhibitor ABBV-075 McDaniel, Keith; Le Wang; Sheppard, George; Fidanze, Steve; Pratt, John; Liu, Dachun; Hasvold, Lisa; Mantei, Robert; Park, Chang; Sarthy, Aparna; Li, Leiming; Albert, Daniel H.; Lin, Xiaoyu; Warder, Scott; Faivre, Emily; Bui, Mai H.; Huang, Xiaoli; Wilcox, Denise; Wang, Rongqi; Magoc, Terry; Rajaraman, Ganesh; Petros, Andrew; Panchal, Sanjay; Sun, Chaohong; Fang, Guowei; Elmore, Steven W.; Rosenberg, Saul; Shen, Yu; Kati, Warren 分享 收藏
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