An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells von Vinogradova, Maia, Gehling, Victor S, Gustafson, Amy, Arora, Shilpi, Tindell, Charles A, Wilson, Catherine, Williamson, Kaylyn E, Guler, Gulfem D, Gangurde, Pranoti, Manieri, Wanda, Busby, Jennifer, Flynn, E Megan, Lan, Fei, Kim, Hyo-jin, Odate, Shobu, Cochran, Andrea G, Liu, Yichin, Wongchenko, Matthew, Yang, Yibin, Cheung, Tommy K, Maile, Tobias M, Lau, Ted, Costa, Michael, Hegde, Ganapati V, Jackson, Erica, Pitti, Robert, Arnott, David, Bailey, Christopher, Bellon, Steve, Cummings, Richard T, Albrecht, Brian K, Harmange, Jean-Christophe, Kiefer, James R, Trojer, Patrick, Classon, Marie

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Identification of (R)‑N‑((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)‑1H‑indole-3-carboxamide (CPI-1205),... von Vaswani, Rishi G, Gehling, Victor S, Dakin, Les A, Cook, Andrew S, Nasveschuk, Christopher G, Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C, Campbell, Robert, Lee, Christina, Cantone, Nico, Cummings, Richard T, Normant, Emmanuel, Bellon, Steven F, Albrecht, Brian K, Harmange, Jean-Christophe, Trojer, Patrick, Audia, James E, Zhang, Ying, Justin, Neil, Chen, Shuyang, Wilson, Jon R, Gamblin, Steven J

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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials von Albrecht, Brian K, Gehling, Victor S, Hewitt, Michael C, Vaswani, Rishi G, Côté, Alexandre, Leblanc, Yves, Nasveschuk, Christopher G, Bellon, Steve, Bergeron, Louise, Campbell, Robert, Cantone, Nico, Cooper, Michael R, Cummings, Richard T, Jayaram, Hariharan, Joshi, Shivangi, Mertz, Jennifer A, Neiss, Adrianne, Normant, Emmanuel, O’Meara, Michael, Pardo, Eneida, Poy, Florence, Sandy, Peter, Supko, Jeffrey, Sims, Robert J, Harmange, Jean-Christophe, Taylor, Alexander M, Audia, James E

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Effects of pH and Low Density Lipoprotein (LDL) on PCSK9-dependent LDL Receptor Regulation von Fisher, Timothy S., Surdo, Paola Lo, Pandit, Shilpa, Mattu, Marco, Santoro, Joseph C., Wisniewski, Doug, Cummings, Richard T., Calzetta, Alessandra, Cubbon, Rose M., Fischer, Paul A., Tarachandani, Anil, De Francesco, Raffaele, Wright, Samuel D., Sparrow, Carl P., Carfi, Andrea, Sitlani, Ayesha

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Structural and Biochemical Characterization of the Wild Type PCSK9-EGF(AB) Complex and Natural Familial Hypercholesterolemia Mutants von Bottomley, Matthew J., Cirillo, Agostino, Orsatti, Laura, Ruggeri, Lionello, Fisher, Timothy S., Santoro, Joseph C., Cummings, Richard T., Cubbon, Rose M., Lo Surdo, Paola, Calzetta, Alessandra, Noto, Alessia, Baysarowich, Jennifer, Mattu, Marco, Talamo, Fabio, De Francesco, Raffaele, Sparrow, Carl P., Sitlani, Ayesha, Carfí, Andrea

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Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII von Leiting, Barbara, Pryor, KellyAnn D, Wu, Joseph K, Marsilio, Frank, Patel, Reshma A, Craik, Charles S, Ellman, Jonathan A, Cummings, Richard T, Thornberry, Nancy A

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Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains von Taylor, Alexander M, Vaswani, Rishi G, Gehling, Victor S, Hewitt, Michael C, Leblanc, Yves, Audia, James E, Bellon, Steve, Cummings, Richard T, Côté, Alexandre, Harmange, Jean-Christophe, Jayaram, Hari, Joshi, Shivangi, Lora, Jose M, Mertz, Jennifer A, Neiss, Adrianne, Pardo, Eneida, Nasveschuk, Christopher G, Poy, Florence, Sandy, Peter, Setser, Jeremy W, Sims, Robert J, Tang, Yong, Albrecht, Brian K

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Photochemical preparation of a pyridone containing tetracycle: A Jak protein kinase inhibitor von THOMPSON, James E, CUBBON, Rose M, DEMARTINO, Julie A, CUMMINGS, Richard T, WICKER, Linda S, FRANKSHUN, Robert, CUNNINGHAM, Barry R, CAMERON, Patricia M, MEINKE, Peter T, LIVERTON, Nigel, YOUMIN WENG

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Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor von Wilson, Jonathan E., Patel, Gaurav, Patel, Chirag, Brucelle, Francois, Huhn, Annissa, Gardberg, Anna S., Poy, Florence, Cantone, Nico, Bommi-Reddy, Archana, Sims, Robert J., Cummings, Richard T., Levell, Julian R.

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A Peptide-Based Fluorescence Resonance Energy Transfer Assay for Bacillus anthracis Lethal Factor Protease von Cummings, Richard T., Salowe, Scott P., Cunningham, Barry R., Wiltsie, Judyann, Park, Young Whan, Sonatore, Lisa M., Wisniewski, Douglas, Douglas, Cameron M., Hermes, Jeffrey D., Scolnick, Edward M.

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Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition von Ghosh, Srimoyee, Taylor, Alexander, Chin, Melissa, Huang, Hon-Ren, Conery, Andrew R., Mertz, Jennifer A., Salmeron, Andres, Dakle, Pranal J., Mele, Deanna, Cote, Alexandre, Jayaram, Hari, Setser, Jeremy W., Poy, Florence, Hatzivassiliou, Georgia, DeAlmeida-Nagata, Denise, Sandy, Peter, Hatton, Charlie, Romero, F. Anthony, Chiang, Eugene, Reimer, Thornik, Crawford, Terry, Pardo, Eneida, Watson, Venita G., Tsui, Vickie, Cochran, Andrea G., Zawadzke, Laura, Harmange, Jean-Christophe, Audia, James E., Bryant, Barbara M., Cummings, Richard T., Magnuson, Steven R., Grogan, Jane L., Bellon, Steve F., Albrecht, Brian K., Sims, Robert J., Lora, Jose M.

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Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity von Stuckey, Jacob I., Cantone, Nico R., Côté, Alexandre, Arora, Shilpi, Vivat, Valerie, Ramakrishnan, Ashwin, Mertz, Jennifer A., Khanna, Avinash, Brenneman, Jehrod, Gehling, Victor S., Moine, Ludivine, Sims, Robert J., Audia, James E., Trojer, Patrick, Levell, Julian R., Cummings, Richard T.

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Identification of potent, selective KDM5 inhibitors von Gehling, Victor S., Bellon, Steven F., Harmange, Jean-Christophe, LeBlanc, Yves, Poy, Florence, Odate, Shobu, Buker, Shane, Lan, Fei, Arora, Shilpi, Williamson, Kaylyn E., Sandy, Peter, Cummings, Richard T., Bailey, Christopher M., Bergeron, Louise, Mao, Weifeng, Gustafson, Amy, Liu, Yichin, VanderPorten, Erica, Audia, James E., Trojer, Patrick, Albrecht, Brian K.

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Discovery, design, and synthesis of indole-based EZH2 inhibitors von Gehling, Victor S., Vaswani, Rishi G., Nasveschuk, Christopher G., Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C., Campbell, Robert, Lee, Christina, Dakin, Les A., Cook, Andrew S., Gagnon, Alexandre, Harmange, Jean-Christophe, Audia, James E., Cummings, Richard T., Normant, Emmanuel, Trojer, Patrick, Albrecht, Brian K.

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Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time von Khanna, Avinash, Cote, Alexandre, Arora, Shilpi, Moine, Ludivine, Gehling, Victor S., Brenneman, Jehrod, Cantone, Nico, Stuckey, Jacob, Apte, Shruti, Ramakrishnan, Ashwin, Bruderek, Kamil, Bradley, William D., Audia, James E., Cummings, Richard T., Sims, Robert J., Trojer, Patrick, Levell, Julian R.

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PCSK9-binding antibody that structurally mimics the EGF(A) domain of LDL-receptor reduces LDL cholesterol in vivo von Ni, Yan G, Di Marco, Stefania, Condra, Jon H, Peterson, Laurence B, Wang, Weirong, Wang, Fubao, Pandit, Shilpa, Hammond, Holly A, Rosa, Ray, Cummings, Richard T, Wood, Dana D, Liu, Xiaomei, Bottomley, Matthew J, Shen, Xun, Cubbon, Rose M, Wang, Sheng-ping, Johns, Douglas G, Volpari, Cinzia, Hamuro, Lora, Chin, Jayne, Huang, Lingyi, Zhao, Jing Zhang, Vitelli, Salvatore, Haytko, Peter, Wisniewski, Douglas, Mitnaul, Lyndon J, Sparrow, Carl P, Hubbard, Brian, Carfí, Andrea, Sitlani, Ayesha

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Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors von Gehling, Victor S., Mcgrath, John P., Duplessis, Martin, Khanna, Avinash, Brucelle, Francois, Vaswani, Rishi G., Cote, Alexandre, Stuckey, Jacob, Watson, Venita, Cummings, Richard T., Balasubramanian, Srividya, Iyer, Priya, Sawant, Priyanka, Good, Andrew C., Albrecht, Brian K., Harmange, Jean-Christophe, Audia, James E., Bellon, Steven F., Trojer, Patrick, Levell, Julian R.

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Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors von Labadie, Sharada S., Dragovich, Peter S., Cummings, Richard T., Deshmukh, Gauri, Gustafson, Amy, Han, Ning, Harmange, Jean-Christophe, Kiefer, James R., Li, Yue, Liang, Jun, Liederer, Bianca M., Liu, Yichin, Manieri, Wanda, Mao, Wiefeng, Murray, Lesley, Ortwine, Daniel F., Trojer, Patrick, VanderPorten, Erica, Vinogradova, Maia, Wen, Li

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Screening for Small-Molecule Inhibitors of Histone Methyltransferases von Cantone, Nico, Cummings, Richard T., Trojer, Patrick

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EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation von Bradley, William D., Arora, Shilpi, Busby, Jennifer, Balasubramanian, Srividya, Gehling, Victor S., Nasveschuk, Christopher G., Vaswani, Rishi G., Yuan, Chih-Chi, Hatton, Charlie, Zhao, Feng, Williamson, Kaylyn E., Iyer, Priyadarshini, Méndez, Jacqui, Campbell, Robert, Cantone, Nico, Garapaty-Rao, Shivani, Audia, James E., Cook, Andrew S., Dakin, Les A., Albrecht, Brian K., Harmange, Jean-Christophe, Daniels, Danette L., Cummings, Richard T., Bryant, Barbara M., Normant, Emmanuel, Trojer, Patrick

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