Zobrazeno 1 - 10
of 66
pro vyhledávání: '"David J, Edmonds"'
Autor:
Shenping Liu, Ruth F. Sommese, Nicole L. Nedoma, Lucy Mae Stevens, Jason K. Dutra, Liying Zhang, David J. Edmonds, Yang Wang, Michelle Garnsey, Michelle F. Clasquin
Publikováno v:
Nature Communications, Vol 14, Iss 1, Pp 1-14 (2023)
Abstract Hydroxysteroid 17-beta-dehydrogenase 13 (HSD17B13) is a hepatic lipid droplet-associated enzyme that is upregulated in patients with non-alcoholic fatty liver disease. Recently, there have been several reports that predicted loss of function
Externí odkaz:
https://doaj.org/article/749817982a194a3cbe9e946b62e48e24
Autor:
David A. Griffith, David J. Edmonds, Jean-Philippe Fortin, Amit S. Kalgutkar, J. Brent Kuzmiski, Paula M. Loria, Aditi R. Saxena, Scott W. Bagley, Clare Buckeridge, John M. Curto, David R. Derksen, João M. Dias, Matthew C. Griffor, Seungil Han, V. Margaret Jackson, Margaret S. Landis, Daniel Lettiere, Chris Limberakis, Yuhang Liu, Alan M. Mathiowetz, Jayesh C. Patel, David W. Piotrowski, David A. Price, Roger B. Ruggeri, David A. Tess
Publikováno v:
Journal of medicinal chemistry. 65(12)
Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited because they require injection. Herein, we describe the discovery of the orally bioavailable, small-molecule, GLP-1
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff991134db369ff3aa7ceaecc2f6263e
https://pubmed.ncbi.nlm.nih.gov/35647711
https://pubmed.ncbi.nlm.nih.gov/35647711
Autor:
Heather Eng, John Litchfield, David A. Griffith, Manthena V.S. Varma, David A. Tess, David J. Edmonds, Amit S. Kalgutkar
Publikováno v:
Journal of Medicinal Chemistry. 63:11831-11844
Prospective predictions of human hepatic clearance for anionic/zwitterionic compounds, which are oftentimes subjected to transporter-mediated uptake, are challenging in drug discovery. We evaluated the utility of preclinical species, rats and cynomol
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b315b32d6b036df8996fa4fc475172db
https://doi.org/10.1021/acs.jmedchem.0c01033
https://doi.org/10.1021/acs.jmedchem.0c01033
Autor:
Shawn D. Doran, Jana Polivkova, James A. Southers, Scott W. Bagley, Kim Huard, Dilinie P. Fernando, Manthena V.S. Varma, David A. Beebe, David J. Edmonds, Robert L. Dow, Benjamin A. Thuma, Collin Crowley, William P. Esler, Trenton T. Ross, David A. Tess, Mark Niosi, Amit S. Kalgutkar, Jeffrey A. Pfefferkorn, Norimitsu Shirai, David A. Griffith, Shawn Cabral, Andrew H. Smith, Gregg D. Cappon, Vincent Mascitti, Matthew S. Dowling, Andre Shavnya, David Price, Ayman El-Kattan, Aaron C. Smith, Yi-an Bi, Spiros Liras, Xiaojing Helen Yang, Cathy Préville
Publikováno v:
Journal of Medicinal Chemistry. 63:10879-10896
Preclinical and clinical data suggest that acetyl-CoA carboxylase (ACC) inhibitors have the potential to rebalance disordered lipid metabolism, leading to improvements in nonalcoholic steatohepatitis (NASH). Consistent with these observations, first-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07da4330450bd15b2bafcbaadc0cc94b
https://doi.org/10.1021/acs.jmedchem.0c00640
https://doi.org/10.1021/acs.jmedchem.0c00640
Autor:
J. Brent Kuzmiski, João M. Dias, Seungil Han, Chris Limberakis, David Price, David J. Edmonds, John M. Curto, Amit S. Kalgutkar, Daniel J. Lettiere, David A. Tess, Clare Buckeridge, Matthew C. Griffor, David R. Derksen, Alan M. Mathiowetz, Roger B. Ruggeri, Paula M. Loria, Aditi R. Saxena, Scott W. Bagley, Yuhang Liu, Margaret S. Landis, David W. Piotrowski, V. Margaret Jackson, David A. Griffith, Jean-Phillipe Fortin
Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited by the requirement for injection. Here we describe the first effective, orally bioavailable small molecule GLP-1R a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::064b771366df377937229b83ffb7a9bf
https://doi.org/10.1101/2020.09.29.319483
https://doi.org/10.1101/2020.09.29.319483
Autor:
Gregory S. Walker, Kimberly O. Cameron, Janice A. Brown, Daniel W. Kung, Angela Wolford, Heather Eng, Kris A. Borzilleri, Jake Delmore, Jessica Ward, David J. Edmonds, Amit S. Kalgutkar, Russell A. Miller, Tim F. Ryder, Allan R. Reyes, Ravi G. Kurumbail, Matthew F. Calabrese
Publikováno v:
Journal of Medicinal Chemistry. 61:7273-7288
Studies on indole-3-carboxylic acid derivatives as direct activators of human adenosine monophosphate-activated protein kinase (AMPK) α1β1γ1 isoform have culminated in the identification of PF-06409577 (1), PF-06885249 (2), and PF-06679142 (3) as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ffee63fc1363789dacc2904147937fe0
https://doi.org/10.1021/acs.jmedchem.8b00807
https://doi.org/10.1021/acs.jmedchem.8b00807
Autor:
Daniel W. Widlicka, Nathan E. Genung, Jana Polivkova, Daniel W. Kung, Wiglesworth Kristin, Thomas Andrew Brandt, Jun Xiao, Matthew S. Dowling, Yingxin Zhang, Paul M. Herrinton, David J. Edmonds, Todd Zahn, Ka Ning Yip, Colin R. Rose, Qifang Li, Jane Panteleev, Shawn Cabral, Andre Shavnya, Nandell F. Keene, John D. Weaver, Benjamin A. Thuma, Michael Herr, Ian Edmonds, Gary Erik Aspnes, Guoqiang Wang, Philip D. Dent, Dilinie P. Fernando, Aaron C. Smith, Michael G. Vetelino, Sophie Y. Lavergne, Edward L. Conn
Publikováno v:
Organic Process Research & Development. 22:681-696
Indole acids 1, 2, and 3 are potent 5′-adenosine monophosphate-activated protein kinase (AMPK) activators for the potential treatment of diabetic nephropathy. Compounds 1–3 were scaled to supply material for preclinical studies, and indole 3 was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b628a560af69b1edadd146b3a36513be
https://doi.org/10.1021/acs.oprd.8b00059
https://doi.org/10.1021/acs.oprd.8b00059
Autor:
Paul DaSilva-Jardine, Jessica Ward, Katherine Cialdea, Matthew F. Calabrese, Marina Amaro, Harmeet Gandhok, Francis Rajamohan, Alan C. Opsahl, Mara Monetti, Kimberly O. Cameron, Tim Rolph, Eliza Bollinger, Benjamin S. Maciejewski, Ravi G. Kurumbail, Christopher T. Salatto, Timothy M. Coskran, David A. Tess, Aditi Jatkar, Nathan E. Genung, Emily Cokorinos, Allan R. Reyes, Morris J. Birnbaum, Germaine Boucher, John M. Kreeger, Andre Shavnya, David J. Edmonds, Russell A. Miller, Amit S. Kalgutkar
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 361:303-311
Diabetic nephropathy remains an area of high unmet medical need, with current therapies that slow down, but do not prevent, the progression of disease. A reduced phosphorylation state of adenosine monophosphate-activated protein kinase (AMPK) has bee
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f66e0afa566f1f67e7eeedde3c3b2a37
https://doi.org/10.1124/jpet.116.237925
https://doi.org/10.1124/jpet.116.237925
Autor:
Paula M. Loria, Aline Dantas de Araujo, David Price, Adam J. Cotterell, David A. Griffith, Spiros Liras, Timothy A. Hill, David P. Fairlie, Weijun Xu, David R. Derksen, Robert V. Stanton, Fabien Plisson, Huy N. Hoang, Justin M. Mitchell, David J. Edmonds
Publikováno v:
European Journal of Medicinal Chemistry. 127:703-714
Glucagon-like peptide (GLP-1) is an endogenous hormone that induces insulin secretion from pancreatic islets and modified forms are used to treat diabetes mellitus type 2. Understanding how GLP-1 interacts with its receptor (GLP-1R) can potentially l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a1066e3cc401d5d060001151234d3a5
https://doi.org/10.1016/j.ejmech.2016.10.044
https://doi.org/10.1016/j.ejmech.2016.10.044
Autor:
Jane M. Withka, Daniel W. Kung, Russell A. Miller, Matthew S. Dowling, Aaron C. Smith, Angela Wolford, Heather Eng, Janice A. Brown, Jun Xiao, Kris A. Borzilleri, Ravi G. Kurumbail, David J. Edmonds, Jessica Ward, Amit S. Kalgutkar, Colin R. Rose, Tim F. Ryder, Meihua Tu, Dilinie P. Fernando, Emily Cokorinos, David Hepworth, James A. Landro, Kimberly O. Cameron, Matthew F. Calabrese, Christopher T. Salatto, Francis Rajamohan, Andre Shavnya, Markus Boehm, Yuxia Mao, Allan R. Reyes, Richard K. Frisbie, Nicole Caspers, Edward L. Conn, Samit Kumar Bhattacharya
Publikováno v:
Journal of Medicinal Chemistry. 59:8068-8081
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropath
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::635e2459bb078e726c0e9a8f44099dcd
https://doi.org/10.1021/acs.jmedchem.6b00866
https://doi.org/10.1021/acs.jmedchem.6b00866