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Structure-Guided Design of Novel, Potent, and Selective Macrocyclic Plasma Kallikrein Inhibitors Li, Zhe; Partridge, James; Silva-Garcia, Abel; Rademacher, Peter; Betz, Andreas; Xu, Qing; Sham, Hing; Hu, Yunjin; Shan, Yuqing; Liu, Bin; Zhang, Ying; Shi, Haijuan; Xu, Qiong; Ma, Xubo; Zhang, Li Share Save
Selective and Brain-Permeable Polo-like Kinase-2 (Plk-2) Inhibitors That Reduce -Synuclein Phosphorylation in Rat Brain Aubele, Danielle L.; Hom, Roy K.; Adler, Marc; Galemmo, Robert A., Jr.; Bowers, Simeon; Truong, Anh P.; Pan, Hu; Beroza, Paul; Neitz, R. Jeffrey; Yao, Nanhua; Lin, May; Tonn, George; Zhang, Heather; Bova, Michael P.; Ren, Zhao; Tam, Danny; Ruslim, Lany; Baker, Jeanne; Diep, Linnea; Fitzgerald, Kent; Hoffman, Jennifer; Motter, Ruth; Fauss, Donald; Tanaka, Pearl; Dappen, Michael; Jagodzinski, Jacek; Chan, Wayman; Konradi, Andrei W.; Latimer, Lee; Zhu, Yong L.; Sham, Hing L.; Anderson, John P.; Bergeron, Marcelle; Artis, Dean R. Share Save
Discovery of (R)-4-Cyclopropyl-7;8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-Cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): Metabolically Stable γ-Secretase Inhibitors that Selectively Inhibit the Production of Amyloid-β over Notch Probst, Gary; Aubele, Danielle L.; Bowers, Simeon; Dressen, Darren; Garofalo, Albert W.; Horn, Roy K.; Konradi, Andrei W.; Marugg, Jennifer L.; Mattson, Matthew N.; Neitzel, Martin L.; Semko, Chris M.; Sham, Hing L.; Smith, Jenifer; Sun, Minghua; Truong, Anh P.; Ye, Xiaocong M.; Xu, Ying-zi; Dappen, Michael S.; Jagodzinski, Jacek J.; Keim, Pamela S.; Peterson, Brian; Latimer, Lee H.; Quincy, David; Wu, Jing; Goldbach, Erich; Ness, Daniel K.; Quinn, Kevin P.; Sauer, John-Michael; Wong, Karina; Zhang, Hongbin; Zmolek, Wes; Brigham, Elizabeth F.; Kholodenko, Dora; Hu, Kang; Kwong, Grace T.; Lee, Michael; Liao, Anna; Motter, Ruth N.; Sacayon, Patricia; Santiago, Pamela; Willits, Christopher; Bard, Frederique; Bova, Michael P.; Hemphill, Susanna S.; Nguyen, Lam; Ruslim, Lany; Tanaka, Kevin; Tanaka, Pearl; Wallace, William; Yednock, Ted A.; Basi, Guriqbal S. Share Save
Polo-like Kinase 2 (PLK2) Phosphorylates α-Synuclein at Serine 129 in Central Nervous System Inglis, Kelly J.; Chereau, David; Brigham, Elizabeth F.; Chiou, San-San; Schoebel, Susanne; Frigon, Normand L.; Yu, Mei; Caccavello, Russell J.; Nelson, Seth; Motter, Ruth; Wright, Sarah; Chian, David; Santiago, Pamela; Soriano, Ferdie; Ramos, Carla; Powell, Kyle; Goldstein, Jason M.; Babcock, Michael; Yednock, Ted; Bard, Frederique; Basi, Guriqbal S.; Sham, Hing; Chilcote, Tamie J.; McConlogue, Lisa; Griswold-Prenner, Irene; Anderson, John P. Share Save
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor Zhao, Gang; Souers, Andrew J.; Voorbach, Martin; Falls, H. Doug; Droz, Brian; Brodjian, Sevan; Lau, Yau Yi; Iyengar, Rajesh R.; Gao, Ju; Judd, Andrew S.; Waaaw, Seble H.; Ravn, Matthew M.; Engstrom, Kenneth M.; Lynch, John K.; Mulhern, Mathew M.; Freeman, Jennifer; Dayton, Brian D.; Wang, Xiaojun; Grihalde, Nelson; Fry, Dennis; Beno, David W. A.; Marsh, Kennan C.; Su, Zhi; Diaz, Gilbert J.; Collins, Christine A.; Sham, Hing; Reilly, Regina M.; Brune, Michael E.; Kym, Philip R. Share Save
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors Wang, Le; Sullivan, Gerard M.; Hexamer, Laura A.; Hasvold, Lisa A.; Thalji, Reema; Przytulinska, Magdalena; Tao, Zhi-Fu; Li, Gaoquan; Chen, Zehan; Xiao, Zhan; Gu, Wen-Zhen; Xue, John; Bui, Mai-Ha; Merta, Philip; Kovar, Peter; Bouska, Jennifer J.; Zhang, Haiying; Park, Chang; Stewart, Kent D.; Sham, Hing L.; Sowin, Thomas J.; Rosenberg, Saul H.; Lin, Nan-Horng Share Save
Discovery of potent, selective, orally bioavailable Stearoyl-CoA desaturase 1 inhibitors Liu, Gang; Lynch, John K.; Freeman, Jennifer; Liu, Bo; Xin, Zhili; Zhao, Hongyu; Serby, Michael D.; Kym, Philip R.; Suhar, Tom S.; Smith, Harriet T.; Cao, Ning; Yang, Ruojing; Janis, Rich S.; Krauser, Joel A.; Cepa, Steven P.; Beno, David W. A.; Sham, Hing L.; Collins, Christine A.; Surowy, Teresa K.; Camp, Heidi S. Share Save
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors Tong, Yunsong; Claiborne, Akiyo; Stewart, Kent D.; Park, Chang; Kovar, Peter; Chen, Zehan; Credo, Robert B.; Gu, Wen-Zhen; Gwaltney, Stephen L., II; Judge, Russell A.; Zhang, Haiying; Rosenberg, Saul H.; Sham, Hing L.; Sowin, Thomas J.; Lin, Nan-horng Share Save
Modulation of drug resistance by α-tubulin in paclitaxel-resistant human lung cancer cell lines (vol 36, pg 1565, 2000) Han, E. Kyu-Ho; Gehrke, L.; Tahir, S. K.; Credo, R. B.; Cherian, S. P.; Sham, H.; Rosenberg, S. H.; Ng, S.-C. Share Save
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. Share Save
N-{3-[2-(4-Alkoxyphenoxy)thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as acetyl-CoA carboxylase inhibitors -: Improvement of cardiovascular and neurological liabilities via structural modifications Gu, Yu Gui; Weitzberg, Moshe; Clark, Richard F.; Xu, Xiangdong; Li, Qun; Lubbers, Nathan L.; Yang, Yi; Beno, David W. A.; Widomski, Deborah L.; Zhang, Tianyuan; Hansen, T. Matthew; Keyes, Robert F.; Waring, Jeffrey F.; Carroll, Sherry L.; Wang, Xiaojun; Wang, Rongqi; Healan-Greenberg, Christine H.; Blomme, Eric A.; Beutel, Bruce A.; Sham, Hing L.; Camp, Heidi S. Share Save
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11β-hydroxysteroid dehydrogenase type 1 inhibitors Rohde, Jeffrey J.; Pliushchev, Marina A.; Sorensen, Bryan K.; Wodka, Dariusz; Shuai, Qi; Wang, Jiahong; Fung, Steven; Monzon, Katina M.; Chiou, William J.; Pan, Liping; Deng, Xiaoqing; Chovan, Linda E.; Ramaiya, Atul; Mullally, Mark; Henry, Rodger F.; Stolarik, DeAnne F.; Imade, Hovis M.; Marsh, Kennan C.; Beno, David W. A.; Fey, Thomas A.; Droz, Brian A.; Brune, Michael E.; Camp, Heidi S.; Sham, Hing L.; Frevert, Ernst Uli; Jacobson, Peer B.; Link, J. T. Share Save
Selective Chk1 inhibitors differentially sensitize p53-deficient cancer cells to cancer therapeutics Chen, Zehan; Xiao, Zhan; Gul, Wen-zhen; Xue, John; Bui, Mai H.; Kovar, Peter; Li, Gaoquan; Wang, Gary; Tao, Zhi-Fu; Tong, Yunsong; Lin, Nan-Horng; Sham, Hing L.; Wang, Jean Y. J.; Sowin, Thomas J.; Rosenberg, Saul H.; Zhang, Haiying Share Save
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. Share Save
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: Assessment of potency, efficacy, and cardiovascular safety Lynch, John K.; Freeman, Jennifer C.; Judd, Andrew S.; Iyengar, Rajesh; Mulhern, Mathew; Zhao, Gang; Napier, James J.; Wodka, Dariusz; Brodjian, Sevan; Dayton, Brian D.; Falls, Doug; Ogiela, Christopher; Reilly, Regina M.; Campbell, Thomas J.; Polakowski, James S.; Hernandez, Lisa; Marsh, Kennan C.; Shapiro, Robin; Knourek-Segel, Victoria; Droz, Brian; Bush, Eugene; Brune, Michael; Preusser, Lee C.; Fryer, Ryan M.; Reinhart, Glenn A.; Houseman, Kathryn; Diaz, Gilbert; Mikhail, Ann; Limberis, James T.; Sham, Hing L.; Collins, Christine A.; Kym, Philip R. Share Save
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. Share Save
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy) thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors (vol 49, pg 3770, 2006) Gu, Yu Gui; Weitzberg, Moshe; Clark, Richard F.; Xu, Xiangdong; Li, Qun; Zhang, Tianyuan; Hansen, T. Matthew; Liu, Gang; Xin, Zhili; Wang, Xiaojun; Wang, Rongqi; McNally, Teresa; Zinker, Bradley A.; Frevert, Ernst U.; Camp, Heidi S.; Beutel, Bruce A.; Sham, Hing L. Share Save
Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-jun NH2-terminal kinase inhibitors Zhao, Hongyu; Serby, Michael D.; Xin, Zhili; Szczepankiewicz, Bruce G.; Liu, Mei; Kosogof, Christi; Liu, Bo; Nelson, Lissa T. J.; Johnson, Eric F.; Wang, Sanyi; Pederson, Terry; Gum, Rebecca J.; Clampit, Jill E.; Haasch, Deanna L.; Abad-Zapatero, Cele; Fry, Elizabeth H.; Rondinone, Cristina; Trevillyan, James M.; Sham, Hing L.; Liu, Gang Share Save
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