Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
Faivre, Emily J., McDaniel, Keith F., Albert, Daniel H., Mantena, Srinivasa R., Plotnik, Joshua P., Wilcox, Denise, Zhang, Lu, Bui, Mai H., Sheppard, George S., Wang, Le, Sehgal, Vasudha, Lin, Xiaoyu, Huang, Xiaoli, Lu, Xin, Uziel, Tamar, Hessler, Paul, Lam, Lloyd T., Bellin, Richard J., Mehta, Gaurav, Fidanze, Steve, Pratt, John K., Liu, Dachun, Hasvold, Lisa A., Sun, Chaohong, Panchal, Sanjay C., Nicolette, John J., Fossey, Stacey L., Park, Chang H., Longenecker, Kenton, Bigelow, Lance, Torrent, Maricel, Rosenberg, Saul H., Kati, Warren M., Shen, Yu
Published in Nature (London) (13.02.2020)
Published in Nature (London) (13.02.2020)
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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
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -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
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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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
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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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
Published in Cancer research (Chicago, Ill.) (01.06.2017)
Published in Cancer research (Chicago, Ill.) (01.06.2017)
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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
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
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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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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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
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Journal Article
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
Fidanze, Steven D., Liu, Dachun, Mantei, Robert A., Hasvold, Lisa A., Pratt, John K., Sheppard, George S., Wang, Le, Holms, James H., Dai, Yujia, Aguirre, Ana, Bogdan, Andrew, Dietrich, Justin D., Marjanovic, Jasmina, Park, Chang H., Hutchins, Charles W., Lin, Xiaoyu, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise, Li, Leiming, Wang, Rongqi, Kovar, Peter, Magoc, Terrance J., Rajaraman, Ganesh, Albert, Daniel H., Shen, Yu, Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Journal Article
Methylpyrrole inhibitors of BET bromodomains
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.
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
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Imidazo[2,1- b]thiazoles: Multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases
Fidanze, Steve D., Erickson, Scott A., Wang, Gary T., Mantei, Robert, Clark, Richard F., Sorensen, Bryan K., Bamaung, Nwe Y., Kovar, Peter, Johnson, Eric F., Swinger, Kerren K., Stewart, Kent D., Zhang, Qian, Tucker, Lora A., Pappano, William N., Wilsbacher, Julie L., Wang, Jieyi, Sheppard, George S., Bell, Randy L., Davidsen, Steven K., Hubbard, Robert D.
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
Published in Bioorganic & medicinal chemistry letters (15.04.2010)
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Journal Article
Physiologically Relevant Metal Cofactor for Methionine Aminopeptidase-2 Is Manganese
Wang, Jieyi, Sheppard, George S, Lou, Pingping, Kawai, Megumi, Park, Chang, Egan, David A, Schneider, Andrew, Bouska, Jennifer, Lesniewski, Rick, Henkin, Jack
Published in Biochemistry (Easton) (06.05.2003)
Published in Biochemistry (Easton) (06.05.2003)
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Journal Article
Correction to 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 (14.05.2015)
Published in Journal of medicinal chemistry (14.05.2015)
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Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605
Pappano, William N, Jung, Paul M, Meulbroek, Jonathan A, Wang, Yi-Chun, Hubbard, Robert D, Zhang, Qian, Grudzien, Meagan M, Soni, Niru B, Johnson, Eric F, Sheppard, George S, Donawho, Cherrie, Buchanan, Fritz G, Davidsen, Steven K, Bell, Randy L, Wang, Jieyi
Published in BMC cancer (04.09.2009)
Published in BMC cancer (04.09.2009)
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Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases
WANG, Gary T, MANTEI, Robert A, BOUSKA, Jennifer, JIEYI WANG, DAVIDSEN, Steven K, BELL, Randy L, SHEPPARD, George S, HUBBARD, Robert D, WILSBACHER, Julie L, QIAN ZHANG, TUCKER, Lora, XIAOMING HU, KOVAR, Peter, JOHNSON, Eric F, OSTERLING, Donald J
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
Published in Bioorganic & medicinal chemistry letters (15.10.2010)
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Journal Article
Discovery and Optimization of Anthranilic Acid Sulfonamides as Inhibitors of Methionine Aminopeptidase-2: A Structural Basis for the Reduction of Albumin Binding
Sheppard, George S, Wang, Jieyi, Kawai, Megumi, Fidanze, Steve D, BaMaung, Nwe Y, Erickson, Scott A, Barnes, David M, Tedrow, Jason S, Kolaczkowski, Lawrence, Vasudevan, Anil, Park, David C, Wang, Gary T, Sanders, William J, Mantei, Robert A, Palazzo, Fabio, Tucker-Garcia, Lora, Lou, Pingping, Zhang, Qian, Park, Chang H, Kim, Ki H, Petros, Andrew, Olejniczak, Edward, Nettesheim, David, Hajduk, Phillip, Henkin, Jack, Lesniewski, Richard, Davidsen, Steven K, Bell, Randy L
Published in Journal of medicinal chemistry (29.06.2006)
Published in Journal of medicinal chemistry (29.06.2006)
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Journal Article
Insulin-like Growth Factor-1 Receptor and ErbB Kinase Inhibitor Combinations Block Proliferation and Induce Apoptosis through Cyclin D1 Reduction and Bax Activation
Wilsbacher, Julie L., Zhang, Qian, Tucker, Lora A., Hubbard, Robert D., Sheppard, George S., Bamaung, Nwe Y., Fidanze, Steve D., Wang, Gary T., Hu, Xiaoming, Davidsen, Steven K., Bell, Randy L., Wang, Jieyi
Published in The Journal of biological chemistry (29.08.2008)
Published in The Journal of biological chemistry (29.08.2008)
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Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor
Wang, Jieyi, Tucker, Lora A, Stavropoulos, Jason, Zhang, Qian, Wang, Yi-Chun, Bukofzer, Gail, Niquette, Amanda, Meulbroek, Jonathan A, Barnes, David M, Shen, Jianwei, Bouska, Jennifer, Donawho, Cherrie, Sheppard, George S, Bell, Randy L
Published in Proceedings of the National Academy of Sciences - PNAS (12.02.2008)
Published in Proceedings of the National Academy of Sciences - PNAS (12.02.2008)
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Discovery, Identification, and Characterization of Candidate Pharmacodynamic Markers of Methionine Aminopeptidase-2 Inhibition
Warder, Scott E, Tucker, Lora A, McLoughlin, Shaun M, Strelitzer, Tamara J, Meuth, Joseph L, Zhang, Qian, Sheppard, George S, Richardson, Paul L, Lesniewski, Rick, Davidsen, Steven K, Bell, Randy L, Rogers, John C, Wang, Jieyi
Published in Journal of proteome research (01.11.2008)
Published in Journal of proteome research (01.11.2008)
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Journal Article
Methionine Aminopeptidase 2 Inhibition Is an Effective Treatment Strategy for Neuroblastoma in Preclinical Models
Morowitz, Michael J, Barr, Rosalind, Wang, Qun, King, Rebecca, Rhodin, Nicholas, Pawel, Bruce, Zhao, Huaqing, Erickson, Scott A, Sheppard, George S, Wang, Jieyi, Maris, John M, Shusterman, Suzanne
Published in Clinical cancer research (01.04.2005)
Published in Clinical cancer research (01.04.2005)
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