HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues
Lin, Xiaoyu, Huang, Xiaoli, Uziel, Tamar, Hessler, Paul, Albert, Daniel H, Roberts-Rapp, Lisa A, McDaniel, Keith F, Kati, Warren M, Shen, Yu
Published in Molecular cancer therapeutics (01.02.2017)
Published in Molecular cancer therapeutics (01.02.2017)
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Identification of Highly Potent Human Immunodeficiency Virus Type‑1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine
Hidaka, Koushi, Kimura, Tooru, Sankaranarayanan, Rajesh, Wang, Jun, McDaniel, Keith F, Kempf, Dale J, Kameoka, Masanori, Adachi, Motoyasu, Kuroki, Ryota, Nguyen, Jeffrey-Tri, Hayashi, Yoshio, Kiso, Yoshiaki
Published in Journal of medicinal chemistry (28.06.2018)
Published in Journal of medicinal chemistry (28.06.2018)
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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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In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir
Ng, Teresa I, Tripathi, Rakesh, Reisch, Thomas, Lu, Liangjun, Middleton, Timothy, Hopkins, Todd A, Pithawalla, Ron, Irvin, Michelle, Dekhtyar, Tatyana, Krishnan, Preethi, Schnell, Gretja, Beyer, Jill, McDaniel, Keith F, Ma, Jun, Wang, Guoqiang, Jiang, Li-Juan, Or, Yat Sun, Kempf, Dale, Pilot-Matias, Tami, Collins, Christine
Published in Antimicrobial agents and chemotherapy (01.01.2018)
Published in Antimicrobial agents and chemotherapy (01.01.2018)
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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-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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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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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
Published in Molecular cancer therapeutics (01.10.2021)
Published in Molecular cancer therapeutics (01.10.2021)
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Novel Physics-Based Ensemble Modeling Approach That Utilizes 3D Molecular Conformation and Packing to Access Aqueous Thermodynamic Solubility: A Case Study of Orally Available Bromodomain and Extraterminal Domain Inhibitor Lead Optimization Series
Hong, Richard S, Mattei, Alessandra, Sheikh, Ahmad Y, Bhardwaj, Rajni Miglani, Bellucci, Michael A, McDaniel, Keith F, Pierce, M. Olivia, Sun, Guangxu, Li, Sizhu, Wang, Lingle, Mondal, Sayan, Ji, Jianguo, Borchardt, Thomas B
Published in Journal of chemical information and modeling (22.03.2021)
Published in Journal of chemical information and modeling (22.03.2021)
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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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Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML
ALBERT, DANIEL H., GOODWIN, NEAL C., DAVIES, ANGELA M., ROWE, JENNY, FEUER, GEROLD, BOYIADZIS, MICHAEL, DORRITIE, KATHLEEN A., MANCINI, MARIA, GANDOUR-EDWARDS, REGINA, JONAS, BRIAN A., BORTHAKUR, GAUTAM, ALDOSS, IBRAHIM, RIZZIERI, DAVID A., ODENIKE, OLATOYOSI, PREBET, THOMAS, SINGH, SANJANA, POPOVIC, RELJA, SHEN, YU, MCDANIEL, KEITH F., KATI, WARREN M., MODI, DIMPLE A., MOTWANI, MONICA, WOLFF, JOHANNES E., FROST, DAVID J.
Published in In vivo (Athens) (01.07.2022)
Published in In vivo (Athens) (01.07.2022)
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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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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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Design and synthesis of pseudo-Symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-Hydrazide isostere
Hidaka, Koushi, Kimura, Tooru, Hayashi, Yoshio, McDaniel, Keith F, Dekhtyar, Tatyana, Colletti, Lynn, Kiso, Yoshiaki
Published in Bioorganic & medicinal chemistry letters (06.01.2003)
Published in Bioorganic & medicinal chemistry letters (06.01.2003)
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Novel Hepatitis C virus replicon inhibitors: Synthesis and structure–activity relationships of fused pyrimidine derivatives
Chris Krueger, A., Madigan, Darold L., Beno, David W., Betebenner, David A., Carrick, Robert, Green, Brian E., He, Wenping, Liu, Dachun, Maring, Clarence J., McDaniel, Keith F., Mo, Hongmei, Molla, Akhteruzzaman, Motter, Christopher E., Pilot-Matias, Tami J., Tufano, Michael D., Kempf, Dale J.
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
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Palladium-catalyzed reactions in the synthesis of 3- and 4-substituted indoles. 2. Total synthesis of the N-acetyl methyl ester of (.+-.)-clavicipitic acids
Harrington, Peter J, Hegedus, Louis S, McDaniel, Keith F
Published in Journal of the American Chemical Society (01.07.1987)
Published in Journal of the American Chemical Society (01.07.1987)
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Inhibitors of HCV NS5B polymerase: synthesis and structure–activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines
Pratt, John K., Donner, Pamela, McDaniel, Keith F., Maring, Clarence J., Kati, Warren M., Mo, Hongmei, Middleton, Tim, Liu, Yaya, Ng, Teresa, Xie, Qinghua, Zhang, Rong, Montgomery, Debra, Molla, Akhteruzzaman, Kempf, Dale J., Kohlbrenner, William
Published in Bioorganic & medicinal chemistry letters (15.03.2005)
Published in Bioorganic & medicinal chemistry letters (15.03.2005)
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Inhibitors of HCV NS5B polymerase: Synthesis and structure–activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring
Rockway, Todd W., Zhang, Rong, Liu, Dachun, Betebenner, David A., McDaniel, Keith F., Pratt, John K., Beno, David, Montgomery, Debra, Jiang, Wen W., Masse, Sherie, Kati, Warren M., Middleton, Tim, Molla, Akhteruzzaman, Maring, Clarence J., Kempf, Dale J.
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
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Synthesis of potent pyrrolidine influenza neuraminidase inhibitors
Krueger, A. Chris, Xu, Yibo, Kati, Warren M., Kempf, Dale J., Maring, Clarence J., McDaniel, Keith F., Molla, Akhteruzzaman, Montgomery, Debra, Kohlbrenner, William E.
Published in Bioorganic & medicinal chemistry (01.03.2008)
Published in Bioorganic & medicinal chemistry (01.03.2008)
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