Delineating the role of cooperativity in the design of potent PROTACs for BTK
Zorba, Adelajda, Nguyen, Chuong, Xu, Yingrong, Starr, Jeremy, Borzilleri, Kris, Smith, James, Zhu, Hongyao, Farley, Kathleen A., Ding, WeiDong, Schiemer, James, Feng, Xidong, Chang, Jeanne S., Uccello, Daniel P., Young, Jennifer A., Garcia-Irrizary, Carmen N., Czabaniuk, Lara, Schuff, Brandon, Oliver, Robert, Montgomery, Justin, Hayward, Matthew M., Coe, Jotham, Chen, Jinshan, Niosi, Mark, Luthra, Suman, Shah, Jaymin C., El-Kattan, Ayman, Qiu, Xiayang, West, Graham M., Noe, Mark C., Shanmugasundaram, Veerabahu, Gilbert, Adam M., Brown, Matthew F., Calabrese, Matthew F.
Published in Proceedings of the National Academy of Sciences - PNAS (31.07.2018)
Published in Proceedings of the National Academy of Sciences - PNAS (31.07.2018)
Get full text
Journal Article
Bax inhibitor‐1 protects from nonalcoholic steatohepatitis by limiting inositol‐requiring enzyme 1 alpha signaling in mice
Lebeaupin, Cynthia, Vallée, Déborah, Rousseau, Déborah, Patouraux, Stéphanie, Bonnafous, Stéphanie, Adam, Gilbert, Luciano, Frederic, Luci, Carmelo, Anty, Rodolphe, Iannelli, Antonio, Marchetti, Sandrine, Kroemer, Guido, Lacas‐Gervais, Sandra, Tran, Albert, Gual, Philippe, Bailly‐Maitre, Béatrice
Published in Hepatology (Baltimore, Md.) (01.08.2018)
Published in Hepatology (Baltimore, Md.) (01.08.2018)
Get full text
Journal Article
A kinetic proofreading model for bispecific protein degraders
Bartlett, Derek W., Gilbert, Adam M.
Published in Journal of pharmacokinetics and pharmacodynamics (01.02.2021)
Published in Journal of pharmacokinetics and pharmacodynamics (01.02.2021)
Get full text
Journal Article
A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors
Lanning, Bryan R, Whitby, Landon R, Dix, Melissa M, Douhan, John, Gilbert, Adam M, Hett, Erik C, Johnson, Theodore O, Joslyn, Chris, Kath, John C, Niessen, Sherry, Roberts, Lee R, Schnute, Mark E, Wang, Chu, Hulce, Jonathan J, Wei, Baoxian, Whiteley, Laurence O, Hayward, Matthew M, Cravatt, Benjamin F
Published in Nature chemical biology (01.09.2014)
Published in Nature chemical biology (01.09.2014)
Get full text
Journal Article
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5-((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli, Dowty, Martin E, Banker, Mary Ellen, Juba, Brian, Jussif, Jason, Lin, Tsung, Vincent, Fabien, Czerwinski, Robert M, Casimiro-Garcia, Agustin, Unwalla, Ray, Trujillo, John I, Liang, Sidney, Balbo, Paul, Che, Ye, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Leung, Louis, Yang, Xin, Soucy, Sarah, Hegen, Martin, Coe, Jotham, Langille, Jonathan, Vajdos, Felix, Chrencik, Jill, Telliez, Jean-Baptiste
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
Get full text
Journal Article
Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors
Flanagan, Mark E, Abramite, Joseph A, Anderson, Dennis P, Aulabaugh, Ann, Dahal, Upendra P, Gilbert, Adam M, Li, Chao, Montgomery, Justin, Oppenheimer, Stacey R, Ryder, Tim, Schuff, Brandon P, Uccello, Daniel P, Walker, Gregory S, Wu, Yan, Brown, Matthew F, Chen, Jinshan M, Hayward, Matthew M, Noe, Mark C, Obach, R. Scott, Philippe, Laurence, Shanmugasundaram, Veerabahu, Shapiro, Michael J, Starr, Jeremy, Stroh, Justin, Che, Ye
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
Get full text
Journal Article
Know your target, know your molecule
Bunnage, Mark E, Gilbert, Adam M, Jones, Lyn H, Hett, Erik C
Published in Nature chemical biology (01.06.2015)
Published in Nature chemical biology (01.06.2015)
Get full text
Journal Article
Inducing protein-protein interactions with molecular glues
Che, Ye, Gilbert, Adam M., Shanmugasundaram, Veerabahu, Noe, Mark C.
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
Get full text
Journal Article
Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes
Schiemer, James, Horst, Reto, Meng, Yilin, Montgomery, Justin I., Xu, Yingrong, Feng, Xidong, Borzilleri, Kris, Uccello, Daniel P., Leverett, Carolyn, Brown, Stephen, Che, Ye, Brown, Matthew F., Hayward, Matthew M., Gilbert, Adam M., Noe, Mark C., Calabrese, Matthew F.
Published in Nature chemical biology (01.02.2021)
Published in Nature chemical biology (01.02.2021)
Get full text
Journal Article
Developing predictive assays: the phenotypic screening "rule of 3"
Vincent, Fabien, Loria, Paula, Pregel, Marko, Stanton, Robert, Kitching, Linda, Nocka, Karl, Doyonnas, Regis, Steppan, Claire, Gilbert, Adam, Schroeter, Thomas, Peakman, Marie-Claire
Published in Science translational medicine (24.06.2015)
Published in Science translational medicine (24.06.2015)
Get more information
Journal Article
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition
Telliez, Jean-Baptiste, Dowty, Martin E, Wang, Lu, Jussif, Jason, Lin, Tsung, Li, Li, Moy, Erick, Balbo, Paul, Li, Wei, Zhao, Yajuan, Crouse, Kimberly, Dickinson, Caitlyn, Symanowicz, Peter, Hegen, Martin, Banker, Mary Ellen, Vincent, Fabien, Unwalla, Ray, Liang, Sidney, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Yang, Xin, Bauman, Jonathan, Trujillo, John I, Casimiro-Garcia, Agustin, Vajdos, Felix F, Leung, Louis, Geoghegan, Kieran F, Quazi, Amira, Xuan, Dejun, Jones, Lyn, Hett, Erik, Wright, Katherine, Clark, James D, Thorarensen, Atli
Published in ACS chemical biology (16.12.2016)
Published in ACS chemical biology (16.12.2016)
Get full text
Journal Article
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation
McAllister, Laura A, Butler, Christopher R, Mente, Scot, O’Neil, Steven V, Fonseca, Kari R, Piro, Justin R, Cianfrogna, Julie A, Foley, Timothy L, Gilbert, Adam M, Harris, Anthony R, Helal, Christopher J, Johnson, Douglas S, Montgomery, Justin I, Nason, Deane M, Noell, Stephen, Pandit, Jayvardhan, Rogers, Bruce N, Samad, Tarek A, Shaffer, Christopher L, da Silva, Rafael G, Uccello, Daniel P, Webb, Damien, Brodney, Michael A
Published in Journal of medicinal chemistry (12.04.2018)
Published in Journal of medicinal chemistry (12.04.2018)
Get full text
Journal Article
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes
Zhang, Yuanjin, Liu, Zhonglin, Hirschi, Marscha, Brodsky, Oleg, Johnson, Eric, Won, Sang Joon, Nagata, Asako, Bezwada, Divya, Petroski, Matthew D, Majmudar, Jaimeen D, Niessen, Sherry, VanArsdale, Todd, Gilbert, Adam M, Hayward, Matthew M, Stewart, Al E, Nager, Andrew R, Melillo, Bruno, Cravatt, Benjamin F
Published in Nature chemical biology (18.09.2024)
Published in Nature chemical biology (18.09.2024)
Get full text
Journal Article
Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms
Leung, Louis, Yang, Xin, Strelevitz, Timothy J, Montgomery, Justin, Brown, Matthew F, Zientek, Michael A, Banfield, Christopher, Gilbert, Adam M, Thorarensen, Atli, Dowty, Martin E
Published in Drug metabolism and disposition (01.01.2017)
Published in Drug metabolism and disposition (01.01.2017)
Get full text
Journal Article
Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes
Schiemer, James, Horst, Reto, Meng, Yilin, Montgomery, Justin I., Xu, Yingrong, Feng, Xidong, Borzilleri, Kris, Uccello, Daniel P., Leverett, Carolyn, Brown, Stephen, Che, Ye, Brown, Matthew F., Hayward, Matthew M., Gilbert, Adam M., Noe, Mark C., Calabrese, Matthew F.
Published in Nature chemical biology (01.02.2021)
Published in Nature chemical biology (01.02.2021)
Get full text
Journal Article
Structure-Based Approach To Identify 5‑[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
Unwalla, Ray, Mousseau, James J, Fadeyi, Olugbeminiyi O, Choi, Chulho, Parris, Kevin, Hu, Baihua, Kenney, Thomas, Chippari, Susan, McNally, Christopher, Vishwanathan, Karthick, Kilbourne, Edward, Thompson, Catherine, Nagpal, Sunil, Wrobel, Jay, Yudt, Matthew, Morris, Carl A, Powell, Dennis, Gilbert, Adam M, Chekler, Eugene L. Piatnitski
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
Get full text
Journal Article
Chiral Sulfoxide-Induced Single Turn Peptide α-Helicity
Zhang, Qingzhou, Jiang, Fan, Zhao, Bingchuan, Lin, Huacan, Tian, Yuan, Xie, Mingsheng, Bai, Guoyun, Gilbert, Adam M., Goetz, Gilles H., Liras, Spiros, Mathiowetz, Alan A., Price, David A., Song, Kun, Tu, Meihua, Wu, Yujie, Wang, Tao, Flanagan, Mark E., Wu, Yun-Dong, Li, Zigang
Published in Scientific reports (09.12.2016)
Published in Scientific reports (09.12.2016)
Get full text
Journal Article