Search Results - "Magoc, Terrance J."

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 by 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

“…The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain…”
Get full text

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 by 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

“…The BET family of proteins consists of BRD2, BRD3, BRD4, and BRDt. Each protein contains two distinct bromodomains (BD1 and BD2). BET family bromodomain…”
Get full text

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy by 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

“…The BCL-2/BCL-XL/BCL-W inhibitor ABT-263 (navitoclax) has shown promising clinical activity in lymphoid malignancies such as chronic lymphocytic leukemia…”
Get more information

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 by 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

“…The development of bromodomain and extraterminal domain (BET) bromodomain inhibitors and their examination in clinical studies, particularly in oncology…”
Get full text

Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia by 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

“…Dual bromodomain BET inhibitors that bind with similar affinities to the first and second bromodomains across BRD2, BRD3, BRD4, and BRDT have displayed modest…”
Get full text

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors by 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

“…Members of the BET family of bromodomain containing proteins have been identified as potential targets for blocking proliferation in a variety of cancer cell…”
Get full text

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors by 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.

“…[Display omitted] •Two novel series of conformationally constrained BET inhibitors have been prepared and characterized.•Compounds in each series demonstrate…”
Get full text

Methylpyrrole inhibitors of BET bromodomains by 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.

“…[Display omitted] An NMR fragment screen for binders to the bromodomains of BRD4 identified 2-methyl-3-ketopyrroles 1 and 2. Elaboration of these fragments…”
Get full text

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor by Albert, Daniel H, Tapang, Paul, Magoc, Terrance J, Pease, Lori J, Reuter, David R, Wei, Ru-Qi, Li, Junling, Guo, Jun, Bousquet, Peter F, Ghoreishi-Haack, Nayereh S, Wang, Baole, Bukofzer, Gail T, Wang, Yi-Chun, Stavropoulos, Jason A, Hartandi, Kresna, Niquette, Amanda L, Soni, Nirupama, Johnson, Eric F, McCall, J Owen, Bouska, Jennifer J, Luo, Yanping, Donawho, Cherrie K, Dai, Yujia, Marcotte, Patrick A, Glaser, Keith B, Michaelides, Michael R, Davidsen, Steven K

“…ABT-869 is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor…”
Get full text

Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families by Glaser, Keith B, Li, Junling, Marcotte, Patrick A, Magoc, Terrance J, Guo, Jun, Reuter, David R, Tapang, Paul, Wei, Ru-Qi, Pease, Lori J, Bui, Mai H, Chen, Zehan, Frey, Robin R, Johnson, Eric F, Osterling, Donald J, Olson, Amanda M, Bouska, Jennifer J, Luo, Yanping, Curtin, Michael L, Donawho, Cherrie K, Michaelides, Michael R, Tse, Chris, Davidsen, Steven K, Albert, Daniel H

“…ABT-348 [1-(4-(4-amino-7-(1-(2-hydroxyethyl)-1H-pyrazol-4-yl)thieno[3,2-c]pyridin-3-yl)phenyl)-3-(3-fluorophenyl)urea] is a novel ATP-competitive multitargeted…”
Get more information

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families by Curtin, Michael L., Frey, Robin R., Heyman, H. Robin, Soni, Niru B., Marcotte, Patrick A., Pease, Lori J., Glaser, Keith B., Magoc, Terrance J., Tapang, Paul, Albert, Daniel H., Osterling, Donald J., Olson, Amanda M., Bouska, Jennifer J., Guan, Zhiwen, Preusser, Lee C., Polakowski, James S., Stewart, Kent D., Tse, Chris, Davidsen, Steven K., Michaelides, Michael R.

“…A series of thienopyridine ureas with dual inhibitory activity against KDR and Aurora B kinase has been identified. Compound 2 (ABT-348) of this series is…”
Get full text

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases by Curtin, Michael L., Robin Heyman, H., Frey, Robin R., Marcotte, Patrick A., Glaser, Keith B., Jankowski, James R., Magoc, Terrance J., Albert, Daniel H., Olson, Amanda M., Reuter, David R., Bouska, Jennifer J., Montgomery, Debra A., Palma, Joann P., Donawho, Cherrie K., Stewart, Kent D., Tse, Chris, Michaelides, Michael R.

“…A series of pyrazole diaminopyrimidines with dual KDR/Aurora B kinase inhibitory activity has been identified. The SAR, physiochemical properties and antitumor…”
Get full text

Discovery and Evaluation of a Series of 3-Acylindole Imidazopyridine Platelet-Activating Factor Antagonists by Curtin, Michael L, Davidsen, Steven K, Heyman, H. Robin, Garland, Robert B, Sheppard, George S, Florjancic, Alan S, Xu, Lianhong, Carrera, George M, Steinman, Douglas H, Trautmann, Jeff A, Albert, Daniel H, Magoc, Terrance J, Tapang, Paul, Rhein, David A, Conway, Richard G, Luo, Gongjin, Denissen, Jon F, Marsh, Kennan C, Morgan, Douglas W, Summers, James B

“…Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and…”
Get full text

N-(Acyloxyalkyl)pyridinium Salts as Soluble Prodrugs of a Potent Platelet Activating Factor Antagonist by Davidsen, Steven K, Summers, James B, Albert, Daniel H, Holms, James H, Heyman, H. Robin, Magoc, Terrance J, Conway, Richard G, Rhein, David A, Carter, George W

“…Pyrrolothiazole 4 is a potent antagonist of platelet activating factor-mediated effects in a variety of in vitro and in vivo assays. Despite its positive…”
Get full text

α-Keto amides as inhibitors of histone deacetylase by Wada, Carol K., Frey, Robin R., Ji, Zhiqin, Curtin, Michael L., Garland, Robert B., Holms, James H., Li, Junling, Pease, Lori J., Guo, Jun, Glaser, Keith B., Marcotte, Patrick A., Richardson, Paul L., Murphy, Shannon S., Bouska, Jennifer J., Tapang, Paul, Magoc, Terrance J., Albert, Daniel H., Davidsen, Steven K., Michaelides, Michael R.

“…α-Keto ester and amides were found to be potent inhibitors of histone deacetylase. Nanomolar inhibitors against the isolated enzyme and sub-micromolar…”
Get full text

Biaryl Ether Retrohydroxamates as Potent, Long-lived, Orally Bioavailable MMP Inhibitors by Michaelides, Michael R., Dellaria, Joseph F., Gong, Jane, Holms, James H., Bouska, Jennifer J., Stacey, Jamie, Wada, Carol K., Heyman, H.Robin, Curtin, Michael L., Guo, Yan, Goodfellow, Carole L., Elmore, Ildiko B., Albert, Daniel H., Magoc, Terrance J., Marcotte, Patrick A., Morgan, Douglas W., Davidsen, Steven K.

“…A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against…”
Get full text

Abstract 800: ABBV-744, a first-in-class and highly selective inhibitor of the second bromodomain of BET family proteins, displays robust activities in preclinical models of acute myelogenous leukemia by Lin, Xiaoyu, Huang, Xiaoli, Bellin, Richard, Faivre, Emily, Hessler, Paul, Lam, Lloyd, Bui, Mai Ha, Wilcox, Denise, Uziel, Tamar, Ferguson, Debra C., Magoc, Terrance J., Albert, Daniel H., McDaniel, Keith F., Kati, Warren, Shen, Yu

“…Many small-molecule inhibitors that target both bromodomains of the BET family proteins (pan BET inhibitors) are undergoing studies in clinical trials…”
Get full text

Abstract 931: Discovery of ABBV-744, a first-in-class highly BDII-selective BET bromodomain inhibitor by 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.

“…The BET family of proteins consists of BRD2, BRD3, BRD4 and BRDT, with each of these proteins containing two distinct bromodomains (BDI and BDII). ABBV-075,…”
Get full text

Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist by Albert, Daniel H., Magoc, Terrance J., Tapang, Paul, Luo, Gongjin, Morgan, Douglas W., Curtin, Michael, Sheppard, George S., Xu, Lianhong, Heyman, H.Robin, Davidsen, Steven K., Summers, James B., Carter, George W.

“…ABT-491 (4-ethynyl- N, N-dimethyl-3-[3-fluoro-4-[(2-methyl-1 H-imidazo-[4,5- c]pyridin-1-yl)methyl]benzoyl]-1 H-indole-1-carboxamide hydrochloride) is a novel…”
Get full text

Methylpyrrole inhibitors of BET bromodomains by 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.

Get full text