Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Oksana C. Palyha"'
Publikováno v:
JCI Insight. 4
Type 2 diabetes mellitus (T2DM), also known as adult-onset diabetes, is characterized by ineffective insulin action due to insulin resistance in key metabolic tissues. Insulin receptor (IR) plays an important role in insulin signal transduction, defe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a827533bc5dd95ecd8c182e2732679b9
https://doi.org/10.1172/jci.insight.124945
https://doi.org/10.1172/jci.insight.124945
Autor:
Jennifer M. Johnston, Karen O. Akinsanya, Jason E. Imbriglio, Noel Byrne, Hratch J. Zokian, Sookhee Ha, Scott P. Salowe, Hyewon Youm, George H. Addona, JeanMarie Lisnock, Vijayalakshmi Agnani, Deborah L. Zink, Kake Zhao, Gregory C. Adam, Yusheng Xiong, Brian K. Hubbard, Pravien Abeywickrema, John P. Caldwell, Yongcheng Huang, Jen Baysarowich, Peter Orth, Wonsuk Chang, Juncai Meng, Michael Kavana, James R. Tata, Whitney Lane Petrilli, Rui Liang, Gopal Parthasarathy, Xi Ai, Rachael E. Ford, Zhe Feng, Oksana C. Palyha, Edward DiNunzio, Stephen M. Soisson, Alison M. Strack, Jennifer M. Shipman, Roman S. Erdmann, Zhijian Lu, Sujata Sharma, Jun Lu
Summary Proprotein convertase substilisin-like/kexin type 9 (PCSK9) is a serine protease involved in a protein-protein interaction with the low-density lipoprotein (LDL) receptor that has both human genetic and clinical validation. Blocking this prot
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::46333ceb2ad6ba949e70430572ed5675
https://doi.org/10.26434/chemrxiv.8800085
https://doi.org/10.26434/chemrxiv.8800085
Autor:
Rui Liang, Xuelei Song, Sheng-Ping Wang, Gino Salituro, Dave G. McLaren, Larissa Wilsie, Ming You, Steven J. Stout, Zhe Feng, Shirly Pinto, Dong-Ming Shen, Ken Marby, Yusheng Xiong, Jim Tata, Timothy He, Andrew K.P. Taggart, Beth Ann Murphy, Margarita Garcia-Calvo, Brian K. Hubbard, Clare London, Oksana C. Palyha, Jason E. Imbriglio, Andreas Verras, Hye Won Youm, Xiaoling Jin, Diana Deckman, Seongah Han, George H. Addona, Qing Chen, Stephen F. Previs, Dan E. Metzger
Publikováno v:
Journal of Medicinal Chemistry. 58:9345-9353
DGAT2 plays a critical role in hepatic triglyceride production, and data suggests that inhibition of DGAT2 could prove to be beneficial in treating a number of disease states. This article documents the discovery and optimization of a selective small
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb381cedc2107c332209df1516f77af9
https://doi.org/10.1021/acs.jmedchem.5b01345
https://doi.org/10.1021/acs.jmedchem.5b01345
Autor:
Aiwu Zhang, Ronald E. Painter, Stephen F. Previs, Shuo Quan, Heather Zhou, Adam B. Weinglass, Anka G. Ehrhardt, Daphne Szeto, Michael Kavana, Sheng-Ping Wang, Dan Xie, Marina Ichetovkin, Brian K. Hubbard, Larissa Wilsie, Karen O. Akinsanya, Thomas P. Roddy, Oksana C Palyha, Jing Xiao, Mark Rosenbach, Alison M. Strack, Donald Chu, Weihua Ni, Douglas Wisniewski, Douglas G. Johns, Jim Milligan, Paul A. Fischer, Sookhee Ha, Xi Ai, George H. Addona, Thomas F. Vogt, Gail Forrest, Jennifer Baysarowich
Publikováno v:
Biochemistry & Molecular Biology Journal.
Human genetics and pharmacologic clinical intervention demonstrate the key role of PCSK9 in cholesterol regulation. To understand the role of the C-terminal domain of PCSK9, two human mutations in this region (S462P and A522T PCSK9) have been profile
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::80bb26633f7235181b008b1018ab1fa7
https://doi.org/10.21767/2471-8084.100026
https://doi.org/10.21767/2471-8084.100026
Autor:
Linda Chang, Yanqing Kan, Alison M. Strack, Yan Guo, Judith N. Gorski, Linus S. Lin, Maria Madeira, Oksana C. Palyha, Thomas J. Lanza, Randy R. Miller, Jasminka Dragovic, Theresa M. Kelly, Ping Liu, Marc L. Reitman, Ravi P. Nargund, Joseph M. Metzger, Harry R. Chobanian, Donald J. Marsh, Kathy Lyons, Jianmei Pang, Kate A. Raustad, Marc D. Chioda, Xiao-Ming Guan, Sheng-Ping Wang
Publikováno v:
ACS Medicinal Chemistry Letters. 3:252-256
Extensive structure-activity relationship studies of a series derived from atropisomer 1, a previously described chiral benzodiazepine sulfonamide series, led to a potent, brain penetrant and selective compound with excellent preclinical pharmacokine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97ff5cc4464b6f25f4e8bebfcd480a62
https://doi.org/10.1021/ml200304j
https://doi.org/10.1021/ml200304j
Autor:
Oksana C. Palyha, Terry D. Faidley, Joseph M. Metzger, Xiao-Ming Guan, Sheng-Ping Wang, Jennifer A. Kosinski, Ravi P. Nargund, Stephanie K. Spann, Marc L. Reitman, Liming Yang, Linus S. Lin, Lauren P. Shearman, Kate A. Raustad, Donald J. Marsh, Kathy Lyons, Theresa M. Kelly, Stephanie Craw, Alison M. Strack, Yanqing Kan, Hong Yu, Jasminka Dragovic, Iyassu K. Sebhat
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 336:356-364
Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated in the regulation of energy homeostasis. Here, we report the biologic effects of a highly optimized BRS-3 agonist, (2S)-1,1,1-trifluoro-2-[4-(1H-pyrazol-1-yl)pheny
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f83aba6c5ca83619726b27f1351081f
https://doi.org/10.1124/jpet.110.174763
https://doi.org/10.1124/jpet.110.174763
Autor:
Marc L. Reitman, Cheng Guo, Theresa M. Kelly, Constantin Tamvakopoulos, Joseph M. Metzger, Tianying Jian, Howard Y. Chen, Arthur A. Patchett, Oksana C. Palyha, Alison M. Strack, Allan J. Goodman, Ravi P. Nargund, Peter H. Dobbelaar, Yanqing Kan, Mark Hadden, Larry Yet, Peter R. Guzzo, Qianping Peng, Linus S. Lin, Shuwen He, Lauren P. Shearman, Alan J. Henderson, Carina P. Tan, Sargent Bruce J, Xiao-Ming Guan, Scott D. Feighner, Iyassu K. Sebhat, Jie Pan, Jian Liu, Donald J. Marsh, Matthew J. Wyvratt, Andrew D. Howard, Megan Ruenz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1913-1917
We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rode
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c9388422b542c24893358d41aa77156
https://doi.org/10.1016/j.bmcl.2010.01.154
https://doi.org/10.1016/j.bmcl.2010.01.154
Autor:
Yongcheng Huang, Jose Castro-Perez, Haihong Zhou, Yusheng Xiong, Oksana C. Palyha, Anthony Ogawa, Xi Ai, Anita Lee, Shirly Pinto, Sookhee Ha, Michael Kavana
Publikováno v:
Circulation. 132
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secreted protein that promotes degradation of cell surface LDL receptors (LDLRs). Decrease in circulating PCSK9 levels by monoclonal antibodies is correlated with improved lipid profiles in h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9d5985cd34d9889571c776d6c66feded
https://doi.org/10.1161/circ.132.suppl_3.15853
https://doi.org/10.1161/circ.132.suppl_3.15853
Autor:
Jiaping Zhang, Andrew K.P. Taggart, Steven J. Stout, Shirly Pinto, Larissa Wilsie, Xun Chen, Xuelei S. Song, David G. McLaren, Jason E. Imbriglio, Margarita Garcia-Calvo, George H. Addona, Christine C. Chung, Lisa M. Sonatore, Oksana C. Palyha
Publikováno v:
Journal of biomolecular screening. 21(2)
Mass spectrometry offers significant advantages over other detection technologies in the areas of hit finding, hit validation, and medicinal chemistry compound optimization. The foremost obvious advantage is the ability to directly measure enzymatic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5a8c17dafb11e5453ff6e2222e4a4bf
https://pubmed.ncbi.nlm.nih.gov/26403520
https://pubmed.ncbi.nlm.nih.gov/26403520
Autor:
Gail Forrest, Michael Wright, Songnian Lin, Jing Chen Xiao, Harry R. Davis, Jose Castro-Perez, Dan Xie, Sheng-Ping Wang, Yusheng Xiong, Kithsiri Herath, Liangsu Wang, Hong-Ping Guan, Samuel S. Engel, Xiaodong Yang, Ku Lu, Li-Ping Sun, David E. Kelley, Daphne Szeto, Mark D. Erion, Stephen F. Previs, Vinit Shah, Paula J. Andryuk, Oksana C. Palyha
Publikováno v:
Journal of Lipid Research, Vol 56, Iss 11, Pp 2183-2195 (2015)
Glucagon and insulin have opposing action in governing glucose homeostasis. In type 2 diabetes mellitus (T2DM), plasma glucagon is characteristically elevated, contributing to increased gluconeogenesis and hyperglycemia. Therefore, glucagon receptor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99e8b509df31d7a3c71abea805913b32
https://pubmed.ncbi.nlm.nih.gov/26373568
https://pubmed.ncbi.nlm.nih.gov/26373568