Výsledky vyhledávání - "Dennis Rentzeperis"

Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes

Autor: Fuyong Du, Brian C. Shook, Karen DiLoreto, Guozhang Xu, Fengbin Song, Yin Liang, Michael David Gaul, Rosie Santulli, Dennis Rentzeperis, Annette Eckardt, Keith T. Demarest, Renee L. DesJarlais

Publikováno v: Bioorganicmedicinal chemistry letters. 29(20)

Type 2 diabetes mellitus (T2DM) is characterized by chronically elevated plasma glucose levels. The inhibition of glucagon-induced hepatic glucose output via antagonism of the glucagon receptor (GCGR) using a small-molecule antagonist is a promising

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b30b8f1be120fa7a91abbdd01da299a
https://pubmed.ncbi.nlm.nih.gov/31519374

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Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists

Autor: Norman D. Huebert, Zhang Rui, Rosie Santulli, Annette Eckardt, Karen DiLoreto, Michael David Gaul, Fengbin Song, Guozhang Xu, Zhao Bao-Ping, Renee L. DesJarlais, Brian C. Shook, Keith T. Demarest, Tianbao Lu, Dennis Rentzeperis

Publikováno v: Bioorganicmedicinal chemistry letters. 29(15)

A novel series of indazole/indole derivatives were discovered as glucagon receptor (GCGR) antagonists through scaffold hopping based on two literature leads: MK-0893 and LY-2409021. Further structure-activity relationship (SAR) exploration and optimi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::170801b02772370463fdfb74991104c7
https://pubmed.ncbi.nlm.nih.gov/31138472

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MBX-102/JNJ39659100, a Novel Peroxisome Proliferator-Activated Receptor-Ligand with Weak Transactivation Activity Retains Antidiabetic Properties in the Absence of Weight Gain and Edema

Autor: Fang Zhang, Dennis Rentzeperis, Francine M. Gregoire, Holly J. Clarke, Brian Edward Lavan, Thomas A. Gustafson, Svetlana Favelyukis, Dorothy D. Sears, L. Edward Clemens, James M. Lenhard, Yi Mu

Publikováno v: Molecular Endocrinology. 23:975-988

MBX-102/JNJ39659100 (MBX-102) is in clinical development as an oral glucose-lowering agent for the treatment of type 2 diabetes. MBX-102 is a nonthiazolidinedione (TZD) selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d5a0582832e3857944e294f2920342f
https://doi.org/10.1210/me.2008-0473

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MBX-102/JNJ39659100, a Novel Peroxisome Proliferator Activated Receptor-γ Ligand with Weak Transactivation Activity Retains Full Anti-Diabetic Properties in the Absence of Side Effects

Autor: Thomas A. Gustafson, Yi Mu, L. Edward Clemens, Francine M. Gregoire, James M. Lenhard, Dorothy D. Sears, Svetlana Favelyukis, Dennis Rentzeperis, Brian Edward Lavan, Fang Zhang, Holly J. Clarke

Publikováno v: The Journal of Clinical Endocrinology & Metabolism. 94:2210-2210

MBX-102/JNJ39659100 (MBX-102) is in clinical development as an oral glucose lowering agent for the treatment of type 2 diabetes. MBX-102 is a non-thiazolidinedione (TZD) selective partial agonist of PPAR-γ that is differentiated from the TZDs struct

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c618b98c459d08f19065b9720a4dca7
https://doi.org/10.1210/jcem.94.6.9995

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