Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Jean M. Whaley"'
Autor:
Simon A. Hinke, Anne M. Cieniewicz, Thomas Kirchner, Katharine D'Aquino, Rupesh Nanjunda, Jason Aligo, Robert Perkinson, Philip Cooper, Ken Boayke, Mark L. Chiu, Steve Jarantow, Eilyn R. Lacy, Yin Liang, Dana L. Johnson, Jean M. Whaley, Russell B. Lingham, Anthony J. Kihm
Publikováno v:
Molecular Metabolism, Vol 10, Iss , Pp 87-99 (2018)
Objective: Insulin resistance is a key feature of Type 2 Diabetes (T2D), and improving insulin sensitivity is important for disease management. Allosteric modulation of the insulin receptor (IR) with monoclonal antibodies (mAbs) can enhance insulin s
Externí odkaz:
https://doaj.org/article/6f1cd4878c614243a31d99d5e43ca832
Autor:
Shu Chang, Anthony V. Azzara, Yi-Xin Li, Marta Dabros, James Kempson, Reshma Panemangelor, Huji Turdi, Kimberly A. Foster, William J. Keim, Jean M. Whaley, Jeffrey A. Robl, Fang Moore, Luping Chen, Mary Jane Cullen, Xiaoping Hou, Atsu Apedo, R. Michael Lawrence, Arvind Mathur, David G. Harden, Wei Meng, Kevin O'Malley, Mary Ann Pelleymounter, Hannguang Chao, Pratik Devasthale, Jon J. Hangeland, Zhengping Ma, Dauh-Rurng Wu, Robert Paul Brigance, Guohua Zhao, Lynn M. Abell, Qi Gao, Susan Harvey, Lisa M. Kopcho, Dong Cheng, Elizabeth A. Dierks, Ching-Hsuen Chu, Suzanne Rooney, Xiang-Yang Ye, Saleem Ahmad, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:14773-14792
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e90999a2854f1a395c0459b5cd876d
https://doi.org/10.1021/acs.jmedchem.1c01356
https://doi.org/10.1021/acs.jmedchem.1c01356
Autor:
Jean M. Whaley, Yin Liang, Ken Boayke, Anthony J. Kihm, Thomas Kirchner, Philip Cooper, Eilyn R. Lacy, Robert Perkinson, Russell B. Lingham, Anne M. Cieniewicz, Steve Jarantow, Rupesh Nanjunda, Jason Aligo, Mark L. Chiu, Simon A. Hinke, Katharine D'Aquino, Dana L. Johnson
Publikováno v:
Molecular Metabolism, Vol 10, Iss, Pp 87-99 (2018)
Molecular Metabolism
Molecular Metabolism
Objective Insulin resistance is a key feature of Type 2 Diabetes (T2D), and improving insulin sensitivity is important for disease management. Allosteric modulation of the insulin receptor (IR) with monoclonal antibodies (mAbs) can enhance insulin se
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0932bb1c1acb8714678b410a3eac47a8
http://www.sciencedirect.com/science/article/pii/S2212877817307950
http://www.sciencedirect.com/science/article/pii/S2212877817307950
Autor:
Yin Liang, Ken Boayke, Simon A. Hinke, Rupesh Nanjunda, Eilyn R. Lacy, Russell B. Lingham, Jean M. Whaley, Dana L. Johnson, Anthony J. Kihm, Philip Cooper, Stephen Jarantow, Mark L. Chiu, Katharine D'Aquino, Robert Perkinson, Anne M. Cieniewicz, Thomas Kirchner
Publikováno v:
Diabetes. 66:206-217
A hallmark of type 2 diabetes is impaired insulin receptor (IR) signaling that results in dysregulation of glucose homeostasis. Understanding the molecular origins and progression of diabetes and developing therapeutics depend on experimental models
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::844cd183a2e575102d46a0e7751948f2
https://doi.org/10.2337/db16-0633
https://doi.org/10.2337/db16-0633
Autor:
Simona Ioja, Xiaojian Zhao, Jean M. Whaley, Saumya Saini, Michael J. Jurczak, Diana K. Costa, Nnamdi Udeh, Richard G. Kibbey
Publikováno v:
Islets
Inhibition of the sodium-glucose co-transporter type 2 (SGLT2) has received growing acceptance as a novel, safe and effective means to improve glycemic control in patients with type 2 diabetes. Inhibition of SGLT2 lowers the renal glucose threshold a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75c68e8f9a66a171c1bc3943dede8a85
https://pubmed.ncbi.nlm.nih.gov/30118626
https://pubmed.ncbi.nlm.nih.gov/30118626
Autor:
Gary G. Cao, Min Zhou, Ramya Jayaram, Douglas B. Moore, Andres S. Hernandez, Tao Wang, Jean M. Whaley, Yue-Zhong Shu, Carrie Xu, Lori Kunselman, Atsu Apedo, William R. Ewing, Reshma Panemangalore, Qi Gao, Arvind Mathur, Richard Rampulla, Bradley A. Zinker, Lauren Haque, Mary Ellen Cvijic, Marta Dabros, Arun Kumar Gupta, Heng Liu, Jeffrey A. Robl, Bruce A. Ellsworth, Jun Shi, Zhengxiang Gu, Jason J. Wilkes, Akin H. Davulcu, Kristin N. Williams, Elizabeth A. Dierks, John Krupinski, Zhenqiu Hong, Edward J. Brady, Ximao Wu, Qin Sun, Hong Cai, Chunshan Xie, Elizabeth A. Jurica, Kimberly A. Foster
Publikováno v:
Journal of medicinal chemistry. 61(3)
G protein-coupled receptor 40 (GPR40) has become an attractive target for the treatment of diabetes since it was shown clinically to promote glucose-stimulated insulin secretion. Herein, we report our efforts to develop highly selective and potent GP
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0fbe81ca0de7013eecb9cd7ee4d58d5d
https://pubmed.ncbi.nlm.nih.gov/29316397
https://pubmed.ncbi.nlm.nih.gov/29316397
Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Autor:
William R. Ewing, Carrie Xu, Heng Liu, Brian J. Murphy, Neil Flynn, Tao Wang, Douglas B. Moore, Lori Kunselman, Bruce A. Ellsworth, Elizabeth A. Jurica, Kimberly A. Foster, Atsu Apedo, Yuan Tian, Yang Hong, Arvind Mathur, Bradley A. Zinker, Biji Jacob, Kristin N. Williams, Min Zhou, Brad D. Maxwell, Gary Cao, Andres S. Hernandez, Qin Sun, Hong Cai, Jean M. Whaley, Elizabeth A. Dierks, Joel C. Barrish, Dora M. Schnur, Ximao Wu, Doree F. Sitkoff, Mary Ellen Cvijic, Richard Rampulla, Chunshan Xie, David S. Nirschl, Reshma Panemangalore, Michael B. Hicks, Jeffrey A. Robl, Jason J. Wilkes
Publikováno v:
Journal of medicinal chemistry. 60(4)
A novel series of pyrrolidine-containing GPR40 agonists is described as a potential treatment for type 2 diabetes. The initial pyrrolidine hit was modified by moving the position of the carboxylic acid, a key pharmacophore for GPR40. Addition of a 4-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::191c75dee9cb5b8c6f860f132f84555d
https://pubmed.ncbi.nlm.nih.gov/28112924
https://pubmed.ncbi.nlm.nih.gov/28112924
Autor:
Michael J. Graziano, Joelle M. Onorato, Timothy P. Reilly, Lynn M. Abell, Jean M. Whaley, Thomas Dorr, Evan B. Janovitz, Deborah Hagan, Mark Tirmenstein
Publikováno v:
International Journal of Toxicology. 32:336-350
Dapagliflozin, a first-in-class, selective inhibitor of sodium-glucose cotransporter 2 (SGLT2), promotes urinary glucose excretion to reduce hyperglycemia for the treatment of type 2 diabetes. A series of nonclinical studies were undertaken to evalua
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::00535fddf6d87e4fd40fcb103cbdf9e4
https://doi.org/10.1177/1091581813505331
https://doi.org/10.1177/1091581813505331
Autor:
Howard Loraine, John N. Feder, Jean M. Whaley, Samantha Ho, Deborah Hagan, Jian Chen, Sandy Williams
Publikováno v:
Diabetes Therapy
SGLT2 (for “Sodium GLucose coTransporter” protein 2) is the major protein responsible for glucose reabsorption in the kidney and its inhibition has been the focus of drug discovery efforts to treat type 2 diabetes. In order to better clarify the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16bb0765fc903a83b5131a9ead770ff7
https://doi.org/10.1007/s13300-010-0006-4
https://doi.org/10.1007/s13300-010-0006-4
Autor:
Claudio Mapelli, Ramakrishna Seethala, Songping Han, Ellen Sieber-McMaster, William R. Ewing, Ashish Khanna, Keith L. Constantine, Douglas James Riexinger, Daniel Longhi, John Krupinski, Zhengping Ma, Constance Smith-Monroy, Bastos Margarita M, Dan Shi, Michael S. Bernatowicz, Joseph R. Taylor, Christine Huang, Rajasree Golla, Gordon William Robinson, Jelka Pluscec, Jean M. Whaley, Sesha Natarajan, Jean-Philippe Meyer, Robert H. Stoffel, Li Xin, Ving G. Lee, Barry Koplowitz, Cecilia L Chi, Ildiko Antal-Zimanyi
Publikováno v:
Journal of Medicinal Chemistry. 52:7788-7799
Glucagon-like peptide 1 (GLP-1) is a 30 or 31 amino acid peptide hormone that contributes to the physiological regulation of glucose homeostasis and food intake. Herein, we report the discovery of a novel class of 11 amino acid GLP-1 receptor agonist
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f59d43fbd51aab4facd89ceaa788aab6
https://doi.org/10.1021/jm900752a
https://doi.org/10.1021/jm900752a