The catalytic mechanism of cyclic GMP‐AMP synthase (cGAS) and implications for innate immunity and inhibition

door Hall, Justin, Ralph, Erik C., Shanker, Suman, Wang, Hong, Byrnes, Laura J., Horst, Reto, Wong, Jimson, Brault, Amy, Dumlao, Darren, Smith, James F., Dakin, Leslie A., Schmitt, Daniel C., Trujillo, John, Vincent, Fabien, Griffor, Matt, Aulabaugh, Ann E.
Gepubliceerd in Protein Sci (2017)

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists

door Liu, Shenping, Dakin, Leslie A., Xing, Li, Withka, Jane M., Sahasrabudhe, Parag V., Li, Wei, Banker, Mary Ellen, Balbo, Paul, Shanker, Suman, Chrunyk, Boris A., Guo, Zuojun, Chen, Jinshan M., Young, Jennifer A., Bai, Guoyun, Starr, Jeremy T., Wright, Stephen W., Bussenius, Joerg, Tan, Sheng, Gopalsamy, Ariamala, Lefker, Bruce A., Vincent, Fabien, Jones, Lyn H., Xu, Hua, Hoth, Lise R., Geoghegan, Kieran F., Qiu, Xiayang, Bunnage, Mark E., Thorarensen, Atli
Gepubliceerd in Sci Rep (2016)

Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay

door Hall, Justin, Brault, Amy, Vincent, Fabien, Weng, Shawn, Wang, Hong, Dumlao, Darren, Aulabaugh, Ann, Aivazian, Dikran, Castro, Dana, Chen, Ming, Culp, Jeffrey, Dower, Ken, Gardner, Joseph, Hawrylik, Steven, Golenbock, Douglas, Hepworth, David, Horn, Mark, Jones, Lyn, Jones, Peter, Latz, Eicke, Li, Jing, Lin, Lih-Ling, Lin, Wen, Lin, David, Lovering, Frank, Niljanskul, Nootaree, Nistler, Ryan, Pierce, Betsy, Plotnikova, Olga, Schmitt, Daniel, Shanker, Suman, Smith, James, Snyder, William, Subashi, Timothy, Trujillo, John, Tyminski, Edyta, Wang, Guoxing, Wong, Jimson, Lefker, Bruce, Dakin, Leslie, Leach, Karen
Gepubliceerd in PLoS One (2017)

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

door 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.
Gepubliceerd in ACS Med Chem Lett (2016)