Histone Modifications and Cancer

Por Audia, James E., Campbell, Robert M.
Publicado no Cold Spring Harb Perspect Biol (2016)

Mentoring Matters in Drug Discovery

Por Blanco, Maria-Jesus, Audia, James E.
Publicado no ACS Med Chem Lett (2020)

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 em 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 no 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 no 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 no 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 no 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 em 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 no 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 no 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 no 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 no 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 no 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 no 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 no 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 no Nat Chem Biol (2015)