Histone Modifications and Cancer

por Audia, James E., Campbell, Robert M.
Publicado en Cold Spring Harb Perspect Biol (2016)

Mentoring Matters in Drug Discovery

por Blanco, Maria-Jesus, Audia, James E.
Publicado en ACS Med Chem Lett (2020)

Ilaprazole and Other Novel Prazole-Based Compounds That Bind Tsg101 Inhibit Viral Budding of Herpes Simplex Virus 1 and 2 and Human Immunodeficiency Virus from Cells

por Leis, Jonathan, Luan, Chi-Hao, Audia, James E., Dunne, Sara F., Heath, Carissa M.
Publicado en J Virol (2021)

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2

por Nasveschuk, Christopher G., Gagnon, Alexandre, Garapaty-Rao, Shivani, Balasubramanian, Srividya, Campbell, Robert, Lee, Christina, Zhao, Feng, Bergeron, Louise, Cummings, Richard, Trojer, Patrick, Audia, James E., Albrecht, Brian K., Harmange, Jean-Christophe P.
Publicado 2014

In Vivo Assessment of Brain Interstitial Fluid with Microdialysis Reveals Plaque-Associated Changes in Amyloid-β Metabolism and Half-Life

por Cirrito, John R., May, Patrick C., O'Dell, Mark A., Taylor, Jennie W., Parsadanian, Maia, Cramer, Jeffrey W., Audia, James E., Nissen, Jeffrey S., Bales, Kelly R., Paul, Steven M., DeMattos, Ronald B., Holtzman, David M.
Publicado en J Neurosci (2003)

Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity

por 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.
Publicado en J Biol Chem (2021)

Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time

por Khanna, Avinash, Côté, Alexandre, Arora, Shilpi, Moine, Ludivine, Gehling, Victor S., Brenneman, Jehrod, Cantone, Nico, Stuckey, Jacob I., Apte, Shruti, Ramakrishnan, Ashwin, Bruderek, Kamil, Bradley, William D., Audia, James E., Cummings, Richard T., Sims, Robert J., Trojer, Patrick, Levell, Julian R.
Publicado en ACS Med Chem Lett (2020)

Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors

por Gehling, Victor S., McGrath, John P., Duplessis, Martin, Khanna, Avinash, Brucelle, Francois, Vaswani, Rishi G., Côté, Alexandre, Stuckey, Jacob, Watson, Venita, Cummings, Richard T., Balasubramanian, Srividya, Iyer, Priyadarshini, Sawant, Priyanka, Good, Andrew C., Albrecht, Brian K., Harmange, Jean-Christophe, Audia, James E., Bellon, Steven F., Trojer, Patrick, Levell, Julian R.
Publicado en ACS Med Chem Lett (2020)

Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors

por Gehling, Victor S., Hewitt, Michael C., Vaswani, Rishi G., Leblanc, Yves, Côté, Alexandre, Nasveschuk, Christopher G., Taylor, Alexander M., Harmange, Jean-Christophe, Audia, James E., Pardo, Eneida, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A., Sims, Robert J., Bergeron, Louise, Bryant, Barbara M., Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Sankaranarayanan, Ravichandran, Yellapantula, Sreegouri, Bangalore Srinivasamurthy, Nandana, Birudukota, Swarnakumari, Albrecht, Brian K.
Publicado 2013

Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains

por 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.
Publicado en ACS Med Chem Lett (2015)

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),...

por 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.
Publicado en J Med Chem (2016)

Robust Central Reduction of Amyloid-β in Humans with an Orally Available, Non-Peptidic β-Secretase Inhibitor

por May, Patrick C., Dean, Robert A., Lowe, Stephen L., Martenyi, Ferenc, Sheehan, Scott M., Boggs, Leonard N., Monk, Scott A., Mathes, Brian M., Mergott, Dustin J., Watson, Brian M., Stout, Stephanie L., Timm, David E., Smith LaBell, Elizabeth, Gonzales, Celedon R., Nakano, Masako, Jhee, Stanford S., Yen, Mark, Ereshefsky, Larry, Lindstrom, Terry D., Calligaro, David O., Cocke, Patrick J., Greg Hall, D., Friedrich, Stuart, Citron, Martin, Audia, James E.
Publicado en J Neurosci (2011)

GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2)

por Crawford, Terry D., Audia, James E., Bellon, Steve, Burdick, Daniel J., Bommi-Reddy, Archana, Côté, Alexandre, Cummings, Richard T., Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael, Huang, Hon-Ren, Jayaram, Hariharan, Jiang, Ying, Joshi, Shivangi, Kiefer, James R., Murray, Jeremy, Nasveschuk, Christopher G., Neiss, Arianne, Pardo, Eneida, Romero, F. Anthony, Sandy, Peter, Sims, Robert J., Tang, Yong, Taylor, Alexander M., Tsui, Vickie, Wang, Jian, Wang, Shumei, Wang, Yongyun, Xu, Zhaowu, Zawadzke, Laura, Zhu, Xiaoqin, Albrecht, Brian K., Magnuson, Steven R., Cochran, Andrea G.
Publicado en ACS Med Chem Lett (2017)

The Potent BACE1 Inhibitor LY2886721 Elicits Robust Central Aβ Pharmacodynamic Responses in Mice, Dogs, and Humans

por May, Patrick C., Willis, Brian A., Lowe, Stephen L., Dean, Robert A., Monk, Scott A., Cocke, Patrick J., Audia, James E., Boggs, Leonard N., Borders, Anthony R., Brier, Richard A., Calligaro, David O., Day, Theresa A., Ereshefsky, Larry, Erickson, Jon A., Gevorkyan, Hykop, Gonzales, Celedon R., James, Douglas E., Jhee, Stanford S., Komjathy, Steven F., Li, Linglin, Lindstrom, Terry D., Mathes, Brian M., Martényi, Ferenc, Sheehan, Scott M., Stout, Stephanie L., Timm, David E., Vaught, Grant M., Watson, Brian M., Winneroski, Leonard L., Yang, Zhixiang, Mergott, Dustin J.
Publicado en J Neurosci (2015)

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition

por 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.
Publicado en J Biol Chem (2016)

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)

por Taylor, Alexander M., Côté, Alexandre, Hewitt, Michael C., Pastor, Richard, Leblanc, Yves, Nasveschuk, Christopher G., Romero, F. Anthony, Crawford, Terry D., Cantone, Nico, Jayaram, Hariharan, Setser, Jeremy, Murray, Jeremy, Beresini, Maureen H., de Leon Boenig, Gladys, Chen, Zhongguo, Conery, Andrew R., Cummings, Richard T., Dakin, Leslie A., Flynn, E. Megan, Huang, Oscar W., Kaufman, Susan, Keller, Patricia J., Kiefer, James R., Lai, Tommy, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Lu, Henry, Pardo, Eneida, Tsui, Vickie, Wang, Jian, Wang, Yongyun, Xu, Zhaowu, Yan, Fen, Yu, Dong, Zawadzke, Laura, Zhu, Xiaoqin, Zhu, Xiaoyu, Sims, Robert J., Cochran, Andrea G., Bellon, Steve, Audia, James E., Magnuson, Steven, Albrecht, Brian K.
Publicado en ACS Med Chem Lett (2016)

The promise and peril of chemical probes

por Arrowsmith, Cheryl H, Audia, James E, Austin, Christopher, Baell, Jonathan, Bennett, Jonathan, Blagg, Julian, Bountra, Chas, Brennan, Paul E, Brown, Peter J, Bunnage, Mark E, Buser-Doepner, Carolyn, Campbell, Robert M, Carter, Adrian J, Cohen, Philip, Copeland, Robert A, Cravatt, Ben, Dahlin, Jayme L, Dhanak, Dashyant, Edwards, Aled M, Frederiksen, Mathias, Frye, Stephen V, Gray, Nathanael, Grimshaw, Charles E, Hepworth, David, Howe, Trevor, Huber, Kilian V M, Jin, Jian, Knapp, Stefan, Kotz, Joanne D, Kruger, Ryan G, Lowe, Derek, Mader, Mary M, Marsden, Brian, Mueller-Fahrnow, Anke, Müller, Susanne, O'Hagan, Ronan C, Overington, John P, Owen, Dafydd R, Rosenberg, Saul H, Ross, Ruth, Roth, Bryan, Schapira, Matthieu, Schreiber, Stuart L, Shoichet, Brian, Sundström, Michael, Superti-Furga, Giulio, Taunton, Jack, Toledo-Sherman, Leticia, Walpole, Chris, Walters, Michael A, Willson, Timothy M, Workman, Paul, Young, Robert N, Zuercher, William J
Publicado en Nat Chem Biol (2015)