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Structural Basis for Achieving GSK-3β Inhibition with High Potency, Selectivity, and Brain Exposure for Positron Emission Tomography Imaging and Drug Discovery Bernard-Gauthier, Vadim; Mossine, Andrew V.; Knight, Ashley; Patnaik, Debasis; Zhao, Wen-Ning; Cheng, Chialin; Krishnan, Hema S.; Xuan, Lucius L.; Chindavong, Peter S.; Reis, Surya A.; Chen, Jinshan Michael; Shao, Xia; Stauff, Jenelle; Arteaga, Janna; Sherman, Phillip; Salem, Nicolas; Bonsall, David; Amaral, Brenda; Varlow, Cassis; Wells, Lisa; Martarello, Laurent; Patel, Shil; Liang, Steven H.; Kurumbail, Ravi G.; Haggarty, Stephen J.; Scott, Peter J. H.; Vasdev, Neil 分享 收藏
Discovery of 3-Cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yObenzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor Related Orphan Receptor C2 Inverse Agonist Schnute, Mark E.; Wennerstal, Mattias; Alley, Jennifer; Bengtsson, Martin; Blinn, James R.; Bolten, Charles W.; Braden, Timothy; Bonn, Tomas; Carlsson, Bo; Caspers, Nicole; Chen, Ming; Choi, Chulho; Collis, Leon P.; Crouse, Kimberly; Farnegardh, Mathias; Fennell, Kimberly F.; Fish, Susan; Flick, Andrew C.; Goos-Nilsson, Annika; Gullberg, Hjalmar; Harris, Peter K.; Heasley, Steven E.; Hegen, Martin; Hromockyj, Alexander E.; Hu, Xiao; Husman, Bolette; Janosik, Tomasz; Jones, Peter; Kaila, Neelu; Kallin, Elisabet; Kauppi, Bjorn; Kiefer, James R.; Knafels, John; Koehler, Konrad; Kruger, Lars; Kurumbail, Ravi G.; Kyne, Robert E., Jr.; Li, Wei; Lofstedt, Joakim; Long, Scott A.; Menard, Carol A.; Mente, Scot; Messing, Dean; Meyers, Marvin J.; Napierata, Lee; Noteberg, Daniel; Nuhant, Philippe; Pelc, Matthew J.; Prinsen, Michael J.; Rhonnstad, Patrik; Backstrom-Rydin, Eva; Sandberg, Johnny; Sandstrom, Maria; Shah, Falgun; Sjoberg, Maria; Sundell, Aron; Taylor, Alexandria P.; Thorarensen, Atli; Trujillo, John I.; Trzupek, John D.; Unwalla, Ray; Vajdos, Felix F.; Weinberg, Robin A.; Wood, David C.; Xing, Li; Zamaratski, Edouard; Zapf, Christoph W.; Zhao, Yajuan; Wilhelmsson, Anna; Berstein, Gabriel 分享 收藏
Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK) Ryder, Tim F.; Calabrese, Matthew F.; Walker, Gregory S.; Cameron, Kimberly O.; Reyes, Allan R.; Borzilleri, Kris A.; Delmore, Jake; Miller, Russell; Kurumbai, Ravi G.; Ward, Jessica; Kung, Daniel W.; Brown, Janice A.; Edmonds, David J.; Eng, Heather; Wolford, Angela C.; Kalgutkar, Amit S. 分享 收藏
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5′-Adenosine Monophosphate-Activated Protein Kinase (AMPK) Edmonds, David J.; Kung, Daniel W.; Kalgutkar, Amit S.; Filipski, Kevin J.; Ebner, David C.; Cabral, Shawn; Smith, Aaron C.; Aspnes, Gary E.; Bhattacharya, Samit K.; Borzilleri, Kris A.; Brown, Janice A.; Calabrese, Matthew F.; Caspers, Nicole L.; Cokorinos, Emily C.; Conn, Edward L.; Dowling, Matthew S.; Eng, Heather; Feng, Bo; Fernando, Dilinie P.; Genung, Nathan E.; Herr, Michael; Kurumbail, Ravi G.; Lavergne, Sophie Y.; Lee, Esther C. -Y.; Li, Qifang; Mathialagan, Sumathy; Miller, Russell A.; Panteleev, Jane; Polivkova, Jana; Rajamohan, Francis; Reyes, Allan R.; Salatto, Christopher T.; Shavnya, Andre; Thuma, Benjamin A.; Tu, Meihua; Ward, Jessica; Withka, Jane M.; Xiao, Jun; Cameron, Kimberly O. 分享 收藏
Rational approach to highly potent and selective apoptosis signal-regulating kinase 1 (ASK1) inhibitors Lovering, Frank; Morgan, Paul; Allais, Christophe; Aulabaugh, Ann; Brodfuehrer, Joanne; Chang, Jeanne; Coe, Jotham; Ding, WeiDong; Dowty, Heather; Fleming, Margaret; Frisbie, Richard; Guzova, Julia; Hepworth, David; Jasti, Jayasankar; Kortum, Steve; Kurumbail, Ravi; Mohan, Shashi; Papaioannou, Nikolaos; Strohbach, Joseph W.; Vincent, Fabien; Lee, Katherine; Zapf, Christoph W. 分享 收藏
Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathys 含ampkβ1亚型的选择性激活可改善糖尿病肾病大鼠模型的肾功能 Salatto, Christopher T.; Miller, Russell A.; Cameron, Kimberly O.; Cokorinos, Emily; Reyes, Allan; Ward, Jessica; Calabrese, Matthew F.; Kurumbail, Ravi G.; Rajamohan, Francis; Kalgutkar, Amit S.; Tess, David A.; Shavnya, Andre; Genung, Nathan E.; Edmonds, David J.; Jatkar, Aditi; Maciejewski, Benjamin S.; Amaro, Marina; Gandhok, Harmeet; Monetti, Mara; Cialdea, Katherine; Bollinger, Eliza; Kreeger, John M.; Coskran, Timothy M.; Opsahl, Alan C.; Boucher, Germaine G.; Birnbaum, Morris J.; DaSilva-Jardine, Paul; Rolph, Tim 分享 收藏
Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice 骨骼肌AMPK的激活促进非人灵长类动物和小鼠的葡萄糖处置和葡萄糖降低 Cokorinos, Emily C.; Delmore, Jake; Reyes, Allan R.; Albuquerque, Bina; Kjobsted, Rasmus; Jorgensen, Nicolas O.; Tran, Jean-Luc; Jatkar, Aditi; Cialdea, Katherine; Esquejo, Ryan M.; Meissen, John; Calabrese, Matthew F.; Cordes, Jason; Moccia, Robert; Tess, David; Salatto, Christopher T.; Coskran, Timothy M.; Opsahl, Alan C.; Flynn, Declan; Blatnik, Matthew; Li, Wenlin; Kindt, Erick; Foretz, Marc; Viollet, Benoit; Ward, Jessica; Kurumbail, Ravi G.; Kalgutkar, Amit S.; Wojtaszewski, Jorgen F. P.; Cameron, Kimberly O.; Miller, Russell A. 分享 收藏
Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy 发现和临床前表征6-氯-5-[4-(1-羟基环丁基) 苯基]-1h-吲哚-3-羧酸 (PF-06409577)，一磷酸腺苷激活的蛋白激酶 (AMPK) 的直接激活剂，用于糖尿病肾病的潜在治疗 Cameron, Kimberly O.; Kung, Daniel W.; Kalgutkar, Amit S.; Kurumbail, Ravi G.; Miller, Russell; Salatto, Christopher T.; Ward, Jessica; Withka, Jane M.; Bhattacharya, Samit K.; Boehm, Markus; Borzilleri, Kris A.; Brown, Janice A.; Calabrese, Matthew; Caspers, Nicole L.; Cokorinos, Emily; Conn, Edward L.; Dowling, Matthew S.; Edmonds, David J.; Eng, Heather; Fernando, Dilinie P.; Frisbie, Richard; Hepworth, David; Landro, James; Mao, Yuxia; Rajamohan, Francis; Reyes, Allan R.; Rose, Colin R.; Ryder, Tim; Shavnya, Andre; Smith, Aaron C.; Tu, Meihua; Wolford, Angela C.; Xiao, Jun 分享 收藏
Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging Liang, Steven H.; Chen, Jinshan Michael; Normandin, Marc D.; Chang, Jeanne S.; Chang, George C.; Taylor, Christine K.; Trapa, Patrick; Plummer, Mark S.; Para, Kimberly S.; Conn, Edward L.; Lopresti-Morrow, Lori; Lanyon, Lorraine F.; Cook, James M.; Richter, Karl E. G.; Nolan, Charlie E.; Schachter, Joel B.; Janat, Fouad; Che, Ye; Shanmugasundaram, Veerabahu; Lefker, Bruce A.; Enerson, Bradley E.; Livni, Elijahu; Wang, Lu; Guehl, Nicolas J.; Patnaik, Debasis; Wagner, Florence F.; Perlis, Roy; Holson, Edward B.; Haggarty, Stephen J.; El Fakhri, Georges; Kurumbail, Ravi G.; Vasdev, Neil 分享 收藏
Probing the enzyme kinetics, allosteric modulation and activation of α1-and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators Rajamohan, Francis; Reyes, Allan R.; Frisbie, Richard K.; Hoth, Lise R.; Sahasrabudhe, Parag; Magyar, Rachelle; Landro, James A.; Withka, Jane M.; Caspers, Nicole L.; Calabrese, Matthew F.; Ward, Jessica; Kurumbail, Ravi G. 分享 收藏
Discovery and Preclinical Profiling of 3-[4-(Morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), A Highly Potent, Selective, Brain Penetrant, and in Vivo Active LRRK2 Kinase Inhibitor Henderson, Jaclyn L.; Kormos, Bethany L.; Hayward, Matthew M.; Coffman, Karen J.; Jasti, Jayasankar; Kurumbail, Ravi G.; Wager, Travis T.; Verhoest, Patrick R.; Noell, G. Stephen; Chen, Yi; Needle, Elie; Berger, Zdenek; Steyn, Stefanus J.; Houle, Christopher; Hirst, Warren D.; Galatsis, Paul 分享 收藏
Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors 变构抑制剂选择性靶向interleukin-2-inducible T细胞激酶的非活性构象 Han, Seungil; Czerwinski, Robert M.; Caspers, Nicole L.; Limburg, David C.; Ding, WeiDong; Wang, Hong; Ohren, Jeffrey F.; Rajamohan, Francis; McLellan, Thomas J.; Unwalla, Ray; Choi, Chulho; Parikh, Mihir D.; Seth, Nilufer; Edmonds, Jason; Phillips, Chris; Shakya, Subarna; Li, Xin; Spaulding, Vikki; Hughes, Samantha; Cook, Andrew; Robinson, Colin; Mathias, John P.; Navratilova, Iva; Medley, Quintus G.; Anderson, David R.; Kurumbail, Ravi G.; Aulabaugh, Ann 分享 收藏
Covalent Inhibitors of Interleukin-2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay Zapf, Christoph W.; Gerstenberger, Brian S.; Xing, Li; Limburg, David C.; Anderson, David R.; Caspers, Nicole; Han, Seungil; Aulabaugh, Ann; Kurumbail, Ravi; Shakya, Subarna; Li, Xin; Spaulding, Vikki; Czerwinski, Robert M.; Seth, Nilufer; Medley, Quintus G. 分享 收藏
Identification of Type-II Inhibitors Using Kinase Structures 使用激酶结构鉴定II型抑制剂 Lovering, Frank; McDonald, Joseph; Whitlock, Gavin A.; Glossop, Paul A.; Phillips, Chris; Bent, Andrew; Sabnis, Yogesh; Ryan, Mark; Fitz, Lori; Lee, Julie; Chang, Jeanne S.; Han, Seungil; Kurumbail, Ravi; Thorarensen, Atli 分享 收藏
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Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship Xie, Jin; Poda, Gennadiy I.; Hu, Yiding; Chen, Natalie X.; Heier, Richard F.; Wolfson, Serge G.; Reding, Matthew T.; Lennon, Patrick J.; Kurumbail, Ravi G.; Selness, Shaun R.; Li, Xiong; Kishore, Nandini N.; Sommers, Cynthia D.; Christine, Lori; Bonar, Sheri L.; Venkatraman, Neetu; Mathialagan, Sumathy; Brustkern, Sarah J.; Huang, Horng-Chih 分享 收藏
Homo-timeric structural model of human microsomal prostaglandin E synthase-1 and characterization of its substrate/inhibitor binding interactions Xing, Li; Kurumbail, Ravi G.; Frazier, Ronald B.; Davies, Michael S.; Fujiwara, Hideji; Weinberg, Robin A.; Gierse, James K.; Caspers, Nicole; Carter, Jeffrey S.; McDonald, Joseph J.; Moore, William M.; Vazquez, Michael L. 分享 收藏
Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase Graneto, Matthew J.; Kurumbail, Ravi G.; Vazquez, Michael L.; Shieh, Huey-Sheng; Pawlitz, Jennifer L.; Williams, Jennifer M.; Stallings, William C.; Geng, Lifeng; Naraian, Ashok S.; Koszyk, Francis J.; Stealey, Michael A.; Xu, Xiangdong D.; Weier, Richard M.; Hanson, Gunnar J.; Mourey, Robert J.; Compton, Robert P.; Mnich, Stephen J.; Anderson, Gary D.; Monahan, Joseph B.; Devraj, Rajesh 分享 收藏
Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) Anderson, David R.; Meyers, Marvin J.; Vernier, William F.; Mahoney, Matthew W.; Kurumbail, Ravi G.; Caspers, Nicole; Poda, Gennadiy I.; Schindler, John F.; Reitz, David B.; Mourey, Robert J. 分享 收藏
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