未登录 Central TYK2 inhibition identifies TYK2 as a key neuroimmune modulator 中枢TYK2抑制确定了TYK2作为关键的神经免疫调节因子 Molitor, Tyler P.; Hayashi, Genki; Lin, Mei-Yao; Dunn, Carissa J.; Peterson, Nathan G.; Poston, Robert G.; Kurnellas, Michael P.; Traver, David A.; Patel, Seona; Akgungor, Zeynep; Leonardi, Virginia; Lewis, Colizel; Segales, Joshua S.; Bennett, Dylan S.; Truong, Anh P.; Dani, Manjari; Naphade, Swati; Wong, Jamie K.; McDermott, Annie E.; Kovalev, Sarah M.; Ciaccio, Gillian L.; Sadiq, Saud A.; Pei, Zhonghua; Wood, Stephen; Rassoulpour, Arash 分享 收藏
In vitro and in vivo characterization of novel MAT2A allosteric inhibitors Pei, Zhonghua; Alam, Muzaffar; Bhola, Neil; Cleary, Leah; Drummond, Jake; Fisher, Marcus; Fleury, Melissa; Garcia, Candy; Givmanesh, Atieh; Xin Linghu; McSpadden, Ethan; Mounir, Zineb; Neilan, Claire; Newby, Zach; Perumal, Senthil; Steel, Richard; Sutton, James; Vaidya, Kedar; Wagle, Marie-Claire; Wang, Jianhong; Yao, Bing; Lackner, Mark; Dillon, Michael P. 分享 收藏
Mat2A Inhibitors decrease growth, increase senescence and p53 stability in MTAP-deleted cancer cells Bhola, Neil; Givmanesh, Atieh; Wagle, Marie-Claire; Garcia, Candy; Vaidya, Kedar; Cleary, Leah; Pei, Zhonghua; Lackner, Mark; Mounir, Zineb 分享 收藏
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors 实施CYP指数设计选择性色氨酸-2,3-双加氧酶抑制剂 Parr, Brendan T.; Pastor, Richard; Sellers, Benjamin D.; Pei, Zhonghua; Jaipuri, Firoz A.; Castanedo, Georgette M.; Gazzard, Lewis; Kumar, Sanjeev; Li, Xiaokai; Liu, Wen; Mendonca, Rohan; Pavana, Roheeth K.; Potturi, Hima; Shao, Cheng; Velvadapu, Venkata; Waldo, Jesse P.; Wu, Guosheng; Yuen, Po-wai; Zhang, Zuhui; Zhang, Yamin; Harris, Seth F.; Oh, Angela J.; DiPasquale, Antonio; Dement, Kevin; La, Hank; Goon, Leanne; Gustafson, Amy; VanderPorten, Erica C.; Mautino, Mario R.; Liu, Yichin 分享 收藏
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2) Pei, Zhonghua; Mendonca, Rohan; Gazzard, Lewis; Pastor, Richard; Goon, Leanne; Gustafson, Amy; VanderPorten, Erica; Hatzivassiliou, Georgia; Dement, Kevin; Cass, Robert; Yuen, Po-wai; Zhang, Yamin; Wu, Guosheng; Lin, Xingyu; Liu, Yichin; Sellers, Benjamin D. 分享 收藏
Linker Immolation Determines Cell Killing Activity of Disulfide-Linked Pyrrolobenzodiazepine Antibody-Drug Conjugates Zhang, Donglu; Pillow, Thomas H.; Ma, Yong; dela Cruz-Chuh, Josefa; Kozak, Katherine R.; Sadowsky, Jack D.; Philips, Gail D. Lewis; Guo, Jun; Darwish, Martine; Fan, Peter; Chen, Jingtian; He, Changrong; Wang, Tao; Yao, Hui; Xu, Zijin; Chen, Jinhua; Wai, John; Pei, Zhonghua; Hop, Cornelis E. C. A.; Khojasteh, S. Cyrus; Dragovich, Peter S. 分享 收藏
Fragment Molecular Orbital Method Applied to Lead Optimization of Novel Interleukin-2 Inducible T-Cell Kinase (ITK) Inhibitors Heifetz, Alexander; Trani, Giancarlo; Aldeghi, Matteo; MacKinnon, Colin H.; McEwan, Paul A.; Brookfield, Frederick A.; Chudyk, Ewa I.; Bodkin, Mike; Pei, Zhonghua; Burch, Jason D.; Ortwine, Daniel F. 分享 收藏
Inhibition of the kinase ITK in a mouse model of asthma reduces cell death and fails to inhibit the inflammatory response Sun, Yonglian; Peng, Ivan; Webster, Joshua D.; Suto, Eric; Lesch, Justin; Wu, Xiumin; Senger, Kate; Francis, George; Barrett, Kathy; Collier, Jenna L.; Burch, Jason D.; Zhou, Meijuan; Chen, Yuan; Chan, Connie; Eastham-Anderson, Jeff; Ngu, Hai; Li, Olga; Staton, Tracy; Havnar, Charles; Jaochico, Allan; Jackman, Janet; Jeet, Surinder; Riol-Blanco, Lorena; Wu, Lawren C.; Choy, David F.; Arron, Joseph R.; McKenzie, Brent S.; Ghilardi, Nico; Ismaili, Moulay Hicham Alaoui; Pei, Zhonghua; DeVoss, Jason; Austin, Cary D.; Lee, Wyne P.; Zarrin, Ali A. 分享 收藏
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo 四氢吲唑作为Interleukin-2诱导型T细胞激酶抑制剂。第二部分。具有增强的体内效力,选择性和药效学调节的第二代类似物 Burch, Jason D.; Barrett, Kathy; Chen, Yuan; DeVoss, Jason; Eigenbrot, Charles; Goldsmith, Richard; Ismaili, M. Hicham A.; Lau, Kevin; Lin, Zhonghua; Ortwine, Daniel F.; Zarrin, Ali A.; McEwan, Paul A.; Barker, John J.; Ellebrandt, Claire; Kordt, Daniel; Stein, Daniel B.; Wang, Xiaolu; Chen, Yong; Hu, Baihua; Xu, Xiaofeng; Yuen, Po-Wai; Zhang, Yamin; Pei, Zhonghua 分享 收藏
Property- and Structure-Guided Discovery of a Tetrahydroindazole Series of Interleukin-2 Inducible T-Cell Kinase Inhibitors Burch, Jason D.; Lau, Kevin; Barker, John J.; Brookfield, Fred; Chen, Yong; Chen, Yuan; Eigenbrot, Charles; Ellebrandt, Claire; Ismaili, M. Hicham A.; Johnson, Adam; Kordt, Daniel; MacKinnon, Colin H.; McEwan, Paul A.; Ortwine, Daniel F.; Stein, Daniel B.; Wang, Xiaolu; Winkler, Dirk; Yuen, Po-Wai; Zhang, Yamin; Zarrin, Ali A.; Pei, Zhonghua 分享 收藏
Pyrimidoaminotropanes as Potent, Selective, and Efficacious Small Molecule Kinase Inhibitors of the Mammalian Target of Rapamycin (mTOR) Estrada, Anthony A.; Shore, Daniel G.; Blackwood, Elizabeth; Chen, Yung-Hsiang; Deshmukh, Gauri; Ding, Xiao; DiPasquale, Antonio G.; Epler, Jennifer A.; Friedman, Lori S.; Koehler, Michael F. T.; Liu, Lichuan; Malek, Shiva; Nonomiya, Jim; Ortwine, Daniel F.; Pei, Zhonghua; Sideris, Steve; St-Jean, Frederic; Trinh, Lan; Truong, Tom; Lyssikatos, Joseph P. 分享 收藏
Potent, Selective, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin Kinase Domain Exhibiting Single Agent Antiproliferative Activity Koehler, Michael F. T.; Bergeron, Philippe; Blackwood, Elizabeth; Bowman, Krista K.; Chen, Yung-Hsiang; Deshmukh, Gauri; Ding, Xiao; Epler, Jennifer; Lau, Kevin; Lee, Leslie; Liu, Lichuan; Ly, Cuong; Malek, Shiva; Nonomiya, Jim; Oeh, Jason; Ortwine, Daniel F.; Sampath, Deepak; Sideris, Steve; Trinh, Lan; Truong, Tom; Wu, Jiansheng; Pei, Zhonghua; Lyssikatos, Joseph P. 分享 收藏
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349 Pei, Zhonghua; Blackwood, Elizabeth; Liu, Lichuan; Malek, Shiva; Belvin, Marcia; Koehler, Michael F. T.; Ortwine, Daniel F.; Chen, Huifen; Cohen, Frederick; Kenny, Jane R.; Bergeron, Philippe; Lau, Kevin; Ly, Cuong; Zhao, Xianrui; Estrada, Anthony A.; Tom Truong; Epler, Jennifer A.; Nonomiya, Jim; Lan Trinh; Sideris, Steve; Lesnick, John; Bao, Linda; Vijapurkar, Ulka; Mukadam, Sophie; Tay, Suzanne; Deshmukh, Gauri; Chen, Yung-Hsiang; Ding, Xiao; Friedman, Lori S.; Lyssikatos, Joseph P. 分享 收藏
mTOR kinase inhibitor potentiates apoptosis of PI3K and MEK inhibitors in diagnostically defined subpopulations Vijapurkar, Ulka; Robillard, Liliane; Zhou, Siqun; Degtyarev, Michael; Lin, Kui; Truong, Tom; Tremayne, Jarrod; Ross, Leanne Berry; Pei, Zhonghua; Friedman, Lori S.; Blackwood, Elizabeth M.; Belvin, Marcia 分享 收藏
Potent, Selective, and Orally Bioavailable Inhibitors of Mammalian Target of Rapamycin (mTOR) Kinase Based on a Quaternary Substituted Dihydrofuropyrimidine Cohen, Frederick; Bergeron, Philippe; Blackwood, Elizabeth; Bowman, Krista K.; Chen, Huifen; DiPasquale, Antonio G.; Epler, Jennifer A.; Koehler, Michael F. T.; Lau, Kevin; Lewis, Cristina; Liu, Lichuan; Ly, Cuong Q.; Malek, Shiva; Nonomiya, Jim; Ortwine, Daniel F.; Pei, Zhonghua; Robarge, Kirk D.; Sideris, Steve; Trinh, Lan; Truong, Tom; Wu, Jiansheng; Zhao, Xianrui; Lyssikatos, Joseph P. 分享 收藏
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors Pei, Zhonghua; Li, Xiaofeng; von Geldern, Thomas W.; Longenecker, Kenton; Pireh, Daisy; Stewart, Kent D.; Backes, Bradley J.; Lai, Chunqiu; Lubben, Thomas H.; Ballaron, Stephen J.; Beno, David W. A.; Kempf-Grote, Anita J.; Sham, Hing L.; Trevillyan, James M. 分享 收藏
Discovery of ((4R,5S)-5-amino-4-(2,4,5-trifluorophenyl)cyclohex-1-enyl)-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes Pei, Zhonghua; Li, Xiaofeng; von Geldern, Thomas W.; Madar, David J.; Longenecker, Kenton; Yong, Hong; Lubben, Thomas H.; Stewart, Kent D.; Zinker, Bradley A.; Backes, Bradley J.; Judd, Andrew S.; Mulhern, Mathew; Ballaron, Stephen J.; Stashko, Michael A.; Mika, Amanda K.; Beno, David W. A.; Reinhart, Glenn A.; Fryer, Ryan M.; Preusser, Lee C.; Kempf-Grote, Anita J.; Sham, Hing L.; Trevillyan, James M. 分享 收藏
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]-4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279):: A very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes Madar, David J.; Kopecka, Hana; Pireh, Daisy; Yong, Hong; Pei, Zhonghua; Li, Xiaofeng; Wiedeman, Paul E.; Djuric, Stevan W.; Von Geldern, Thomas W.; Fickes, Michael G.; Bhagavatula, Lakshmi; McDermott, Todd; Wittenberger, Steven; Richards, Steven J.; Longenecker, Kenton L.; Stewart, Kent D. 分享 收藏
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors. (vol 49, pg 3521, 2006) Pei, Zhonghua; Li, Xiaofeng; Longenecker, Kenton; von Geldern, Thomas W.; Wiedeman, Paul E.; Lubben, Thomas H.; Zinker, Bradley A.; Stewart, Kent; Ballaron, Stephen J.; Stashko, Michael A.; Mika, Amanda K.; Beno, David W. A.; Long, Michelle; Wells, Heidi; Kempf-Grote, Anita J.; Madar, David J.; McDermott, Todd S.; Bhagavatula, Lakshmi; Fickes, Michael G.; Pireh, Daisy; Solomon, Larry R.; Lake, Marc R.; Edalji, Rohinton; Fry, Elizabeth H.; Sham, Hing L.; Trevillyan, James M. 分享 收藏
Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors Pei, Zhonghua; Li, Xiaofeng; Longenecker, Kenton; von Geldern, Thomas W.; Wiedeman, Paul E.; Lubben, Thomas H.; Zinker, Bradley A.; Stewart, Kent; Ballaron, Stephen J.; Stashko, Michael A.; Mika, Amanda K.; Beno, David W. A.; Long, Michelle; Wells, Heidi; Kempf-Grote, Anita J.; Madar, David J.; McDermott, Todd S.; Bhagavatula, Lakshmi; Fickes, Michael G.; Pireh, Daisy; Solomon, Larry R.; Lake, Marc R.; Edalji, Rohinton; Fry, Elizabeth H.; Sham, Hing L.; Trevillyan, James M. 分享 收藏