Zobrazeno 1 - 10
of 17
pro vyhledávání: '"David R. Derksen"'
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:
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:
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:
Justin M. Mitchell, Joakim E. Swedberg, Spiros Liras, Roger B. Ruggeri, David A. Griffith, David J. Edmonds, David P. Fairlie, Paula M. Loria, David Price, David J. Craik, Christina I. Schroeder, Thomas Durek, David R. Derksen
Publikováno v:
European Journal of Medicinal Chemistry. 103:175-184
Type 2 diabetes mellitus (T2DM) results from compromised pancreatic β-cell function, reduced insulin production, and lowered insulin sensitivity in target organs resulting in hyperglycemia. The GLP-1 hormone has two biologically active forms, GLP-1-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4964b67c73c2dc5e67f36a69c5039c1c
https://doi.org/10.1016/j.ejmech.2015.08.046
https://doi.org/10.1016/j.ejmech.2015.08.046
Autor:
Spiros Liras, David W. Piotrowski, David R. Derksen, W. Mei Kok, Timothy A. Hill, David Price, Kun Song, David P. Fairlie, Jacky Y. Suen, Paula M. Loria, David A. Griffith, Jane M. Withka, Alan M. Mathiowetz, David J. Edmonds, Vincent Mascitti, Huy N. Hoang, Chris Limberakis, Justin M. Mitchell, Robert V. Stanton
Publikováno v:
Journal of Medicinal Chemistry. 58:4080-4085
Cyclic constraints are incorporated into an 11-residue analogue of the N-terminus of glucagon-like peptide-1 (GLP-1) to investigate effects of structure on agonist activity. Cyclization through linking side chains of residues 2 and 5 or 5 and 9 produ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5463a16c556b351f45c0945b48f8486
https://doi.org/10.1021/acs.jmedchem.5b00166
https://doi.org/10.1021/acs.jmedchem.5b00166
Autor:
Karen Atkinson, Timothy P. Rolph, Kris A. Borzilleri, Robert J. Aiello, Levenia Baker, Xiayang Qiu, Theresa D’Aquila, Angel Guzman-Perez, Meihua Tu, Xi Song, Jeffrey A. Pfefferkorn, Shenping Liu, David R. Derksen, Boris A. Chrunyk, James A. Landro, John Litchfield, Kevin J. Filipski, Jane M. Withka, Patricia Bourassa, Francis Bourbonais, Nicole Barrucci
Publikováno v:
Med. Chem. Commun.. 5:802-807
Activation of glucokinase represents a promising strategy for the treatment of type 2 diabetes; however, drug candidates have failed in clinical trials due to narrow therapeutic index between glucose-lowering efficacy and hypoglycemia. Described here
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4e8d245e5965543e527636b54f722cb3
https://doi.org/10.1039/c4md00027g
https://doi.org/10.1039/c4md00027g
Autor:
Ketan S. Gajiwala, Dongxiang Zeng, Jeffrey A. Pfefferkorn, Francis Bourbonais, Christopher S. Jones, Michael J. Hickey, Christian Perreault, Paul S. Humphries, Robert John Maguire, Jianwei Bian, Shenping Liu, Kevin J. Filipski, Mary Theresa Didiuk, Meihua Tu, Gary Erik Aspnes, David R. Derksen, Robert L. Dow, Angel Guzman-Perez, Richard F. Hank, Theodore O. Johnson, John Litchfield, John D. Knafels, Karen Atkinson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4571-4578
Glucokinase activators are a class of experimental agents under investigation as a therapy for Type 2 diabetes mellitus. An X-ray crystal structure of a modestly potent agent revealed the potential to substitute the common heterocyclic amide donor–
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d85cc1bead52a2c15a57800675af57c5
https://doi.org/10.1016/j.bmcl.2013.06.036
https://doi.org/10.1016/j.bmcl.2013.06.036
Autor:
Jeffrey A, Pfefferkorn, Meihua, Tu, Kevin J, Filipski, Angel, Guzman-Perez, Jianwei, Bian, Gary E, Aspnes, Matthew F, Sammons, Wei, Song, Jian-Cheng, Li, Christopher S, Jones, Leena, Patel, Tim, Rasmusson, Dongxiang, Zeng, Kapil, Karki, Michael, Hamilton, Richard, Hank, Karen, Atkinson, John, Litchfield, Robert, Aiello, Levenia, Baker, Nicole, Barucci, Patricia, Bourassa, Francis, Bourbonais, Francis, Bourbounais, Theresa, D'Aquila, David R, Derksen, Margit, MacDougall, Alan, Robertson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7100-7105
Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identificatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::decea8e508a8ec84ae478bd0cc878d20
https://doi.org/10.1016/j.bmcl.2012.09.082
https://doi.org/10.1016/j.bmcl.2012.09.082
Autor:
David A. Griffith, David J. Edmonds, Spiros Liras, Roger B. Ruggeri, Christina I. Schroeder, Justin M. Mitchell, Joakim E. Swedberg, David J. Craik, David R. Derksen, David P. Fairlie, David Price, Paula M. Loria
Glucagon-like peptide-1 (GLP-1) signaling through the glucagon-like peptide 1 receptor (GLP-1R) is a key regulator of normal glucose metabolism, and exogenous GLP-1R agonist therapy is a promising avenue for the treatment of type 2 diabetes mellitus.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0acf427e2f74896177155e5036165ddd
https://europepmc.org/articles/PMC4957059/
https://europepmc.org/articles/PMC4957059/
Autor:
Steven B. Coffey, Joel T. Arcari, Paula M. Loria, Esther C.Y. Lee, Kentaro Futatsugi, Raman Sharma, David R. Derksen, Amit S. Kalgutkar, Kevin B. Bahnck
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(11)
Prostaglandin E receptor subtype 3 (EP3) antagonism may treat a variety of symptoms from inflammation to cardiovascular and metabolic diseases. Previously, most EP3 antagonists were large acidic ligands that mimic the substrate, prostaglandin E2 (PGE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3bad0904c90a0e00a80a1a42da09da66
https://pubmed.ncbi.nlm.nih.gov/27107947
https://pubmed.ncbi.nlm.nih.gov/27107947