Zobrazeno 1 - 10
of 46
pro vyhledávání: '"Kirk McPherson"'
Autor:
Laurel Sweet, Carine Beysen, William P. Esler, David Price, Alan M. Mathiowetz, David A. Griffith, Daniel W. Kung, Scott W. Bagley, Scott M. Turner, Gabriele E. Sonnenberg, Eric Ravussin, Santos Carvajal-Gonzalez, Felix Vajdos, Chris Limberakis, James A. Southers, Paul A. Amor, Shawn D. Doran, Kirk McPherson
Publikováno v:
Journal of Medicinal Chemistry
Acetyl-CoA carboxylase (ACC) inhibitors offer significant potential for the treatment of type 2 diabetes mellitus (T2DM), hepatic steatosis, and cancer. However, the identification of tool compounds suitable to test the hypothesis in human trials has
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1aef7fc28748a6cde4608945069cb34
http://europepmc.org/articles/PMC4281100
http://europepmc.org/articles/PMC4281100
Autor:
David J. Edmonds, Shawn D. Doran, Dongxiang Zeng, Elnaz Menhaji-Klotz, Kathrine Loomis, Jana Polivkova, Kevin B. Bahnck, Tereece Banks, Dianna E. Moore, David A. Griffith, James A. Southers, Matthew F. Dunn, Aaron C. Smith, Carmen N. Garcia-Irizarry, Cathy Préville, William P. Esler, Kirk McPherson, Alan M. Mathiowetz, Paul A. Amor, David A. Beebe, Robert L. Dow, Scott W. Bagley, Kim Huard
Publikováno v:
Journal of Medicinal Chemistry. 56:7110-7119
Acetyl-CoA carboxylase (ACC) catalyzes the rate-determining step in de novo lipogenesis and plays a crucial role in the regulation of fatty acid oxidation. Alterations in lipid metabolism are believed to contribute to insulin resistance; thus inhibit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40cff94b0e675bc3976fd9e44bb5a85d
https://doi.org/10.1021/jm401033t
https://doi.org/10.1021/jm401033t
Autor:
Judith L. Treadway, David W. Piotrowski, R. Kirk McPherson, Jana Polivkova, Anne M. Brodeur, Shenping Liu, Bernard Hulin, David D. Boyer, Stephen J. Orena, Xiayang Qiu, Maria A. Vanvolkenburg, Dennis E. Danley, Donald C. Wilder, Janice C. Parker, Shawn D. Doran, Carolyn B. Soglia, Mark Ammirati, Kim M. Andrews
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1991-1995
A series of 4-substituted proline amides was synthesized and evaluated as inhibitors of dipeptidyl pepdidase IV for the treatment of type 2 diabetes. (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fb8cf65715687f0bc8ee1e7e04655a6
https://doi.org/10.1016/j.bmcl.2009.02.041
https://doi.org/10.1016/j.bmcl.2009.02.041
Autor:
Kathrine Loomis, Kristin L. Rockwell, Meihua Tu, Paul A. Amor, Kirk McPherson, William P. Esler, Tereece Banks, Aaron C. Smith, Shawn Cabral, James J. Valentine, Susan Tapley, Kristen Ford, Colin R. Rose, Mark Niosi, Felix Vajdos, Carmen N. Garcia-Irizarry, Shawn D. Doran, James A. Southers, Scott W. Bagley, Margaret S. Landis, Alan M. Mathiowetz, Daniel W. Kung, David A. Griffith
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(22)
A novel series of spirocyclic-diamine based, isoform non-selective inhibitors of acetyl-CoA carboxylase (ACC) is described. These spirodiamine derivatives were discovered by design of a library to mimic the structural rigidity and hydrogen-bonding pa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d97747d7f1eb5d78c33f023f1c9e7174
https://pubmed.ncbi.nlm.nih.gov/26411795
https://pubmed.ncbi.nlm.nih.gov/26411795
Autor:
Hong Wang, Judith L. Treadway, Maria A. Vanvolkenburg, Anne M. Brodeur, L. D. Mcclure, Shawn D. Doran, Jay S. Lillquist, Kim M. Andrews, Stephen J. Orena, Stephen W. Wright, Donald C. Wilder, Jana Polivkova, R. Kirk McPherson, Mark Ammirati, Janice C. Parker, Thanh V. Olson, Walter C. Soeller, Xiayang Qiu, Carolyn B. Soglia, Dennis E. Danley
Publikováno v:
Journal of Medicinal Chemistry. 49:3068-3076
Inhibitors of the glucagon-like peptide-1 (GLP-1) degrading enzyme dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes in animal models and in human subjects. A novel series of cis-2,5-dicyanopyrrolidine al
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7225566352cae2523ca6fd2fce0bf4d9
https://doi.org/10.1021/jm0600085
https://doi.org/10.1021/jm0600085
Autor:
Katherine Loomis, Kevin Daniel Freeman-Cook, Zhengrong Zhao, Susan Tapley, Dennis Paul Phillion, Richard L. Elliott, Steven B. Coffey, Christopher S. Jones, Kevin E. Henegar, Kirk McPherson, Chris Limberakis, Scott Bader, Janet A. Houser, Leanne M. Buzon, Angel Guzman-Perez, Shawn D. Doran, Wei Song, Betsy Pierce, Kendra Louise Nelson, Meihua Tu, William P. Esler, Kenneth J. DiRico, Sharad B. Murdande, Jeffrey W. Corbett, Paul A. Amor, Eliot Sugarman
Publikováno v:
Journal of medicinal chemistry. 55(2)
This paper describes the design and synthesis of a novel series of dual inhibitors of acetyl-CoA carboxylase 1 and 2 (ACC1 and ACC2). Key findings include the discovery of an initial lead that was modestly potent and subsequent medicinal chemistry op
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25c9f7d939bcab8b1a7e28a3e8df0533
https://pubmed.ncbi.nlm.nih.gov/22148323
https://pubmed.ncbi.nlm.nih.gov/22148323
Autor:
Tara B. Manion, Michael Patrick Pence, Jennifer L. LaPerle, David W. Piotrowski, Susan Tapley, Paul DaSilva-Jardine, R. Kirk McPherson, Robert L. Dow, Angel Guzman-Perez, William J. Zavadoski, Gregory S. Walker, E. Michael Gibbs, Jian-Cheng Li, John Litchfield, Eliot Sugarman, Michael John Munchhof
Publikováno v:
ACS medicinal chemistry letters. 2(5)
Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides. DGAT-1 knockout mice have been shown to be resistant to diet-induced obesity and have increased insulin sensitivity. Thus, inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8293e8fce98fd024b807c1aee4957c08
https://pubmed.ncbi.nlm.nih.gov/24900321
https://pubmed.ncbi.nlm.nih.gov/24900321
Publikováno v:
Metabolism. 42:1583-1587
We examined effects of a novel antidiabetic agent, racemic englitazone (CP 68,722, Pfizer), on normal rat hepatocytes in vitro. For optimal effects, CP 68,722 must be preincubated for approximately 20 minutes. CP 68,722 inhibited the actions of gluca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c69eced6244c3a66d2bdb5b5496c9e6
https://doi.org/10.1016/0026-0495(93)90154-g
https://doi.org/10.1016/0026-0495(93)90154-g
Autor:
H. James Harwood, R. Kirk McPherson, Susan Tapley, Leanne M. Buzon, Kevin Daniel Freeman-Cook, Steven B. Coffey, Richard L. Elliott, Darcy Kohls, Liang Tong, Felix Vajdos, Meihua Tu, Eliot Sugarman, Shawn D. Doran, Francis Rajamohan, Eric S. Marr, Hailong Zhang, Wei Song, Kenneth J. DiRico, Jeffrey W. Corbett, Janet A. Houser, Sharad B. Murdande, William P. Esler, Martha L. Minich, Christopher J. Jones
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(7)
Screening Pfizer's compound library resulted in the identification of weak acetyl-CoA carboxylase inhibitors, from which were obtained rACC1 CT-domain co-crystal structures. Utilizing HTS hits and structure-based drug discovery, a more rigid inhibito
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c15f1a6bcbbc031e2169b1cbccc4dfb
https://pubmed.ncbi.nlm.nih.gov/20219367
https://pubmed.ncbi.nlm.nih.gov/20219367
Autor:
Maria A. Vanvolkenburg, L. D. Mcclure, Stephen J. Orena, Kim M. Andrews, Benjamin N. Rocke, Jay S. Lillquist, Judith L. Treadway, Stephen W. Wright, Zhengrong Zhao, Thanh V. Olson, Janice C. Parker, Shawn D. Doran, Walter C. Soeller, R. Kirk McPherson, Anne M. Brodeur, Cox Eric David, Carolyn B. Soglia, Shenping Liu, Mark Ammirati, Dennis E. Danley
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(20)
A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identif
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69f927a94060b522e9278cf93b62b98b
https://pubmed.ncbi.nlm.nih.gov/17822893
https://pubmed.ncbi.nlm.nih.gov/17822893