Results 191 to 200 of about 2,748,395 (254)

Structure of the glucagon receptor in complex with a glucagon analogue

Nature, 2018
Class B G-protein-coupled receptors (GPCRs), which consist of an extracellular domain (ECD) and a transmembrane domain (TMD), respond to secretin peptides to play a key part in hormonal homeostasis, and are important therapeutic targets for a variety of diseases.
Haonan Zhang, A. Qiao, Linlin Yang, N. Eps, K. S. Frederiksen, Dehua Yang, A. Dai, Xiao-qing Cai, Hui Zhang, C. Yi, C. Cao, Lingli He, Huaiyu Yang, J. Lau, O. Ernst, M. Hanson, R. Stevens, Ming-Wei Wang, S. Reedtz-Runge, Hualiang Jiang, Qiang Zhao, Beili Wu   +21 more
semanticscholar   +3 more sources

Structural basis of Gs and Gi recognition by the human glucagon receptor

Science, 2020
Choosing a partner that fits G protein–coupled receptors (GPCRs) are responsible for transducing diverse signals from outside to inside cells. This process requires specificity both in ligand binding to GPCRs and in coupling between GPCRs and their ...
A. Qiao, Shuo Han, Xinmei Li, Zhixin Li, P. Zhao, A. Dai, Rulve Chang, L. Tai, Q. Tan, Xiaojing Chu, Limin Ma, T. Thorsen, S. Reedtz-Runge, Dehua Yang, Ming-Wei Wang, P. Sexton, D. Wootten, F. Sun, Qiang Zhao, Beili Wu   +19 more
semanticscholar   +1 more source

Amino acids are sensitive glucagon receptor‐specific biomarkers for glucagon‐like peptide‐1 receptor/glucagon receptor dual agonists

Diabetes, Obesity and Metabolism, 2020
Abstract Aim The aim of this study was to evaluate amino acids as glucagon receptor (GCGR)‐specific biomarkers in rodents and cynomolgus monkeys in the presence of agonism of both glucagon‐like peptide‐1 receptor (GLP1R) and GCGR with a variety of dual agonist compounds.
Wenyu Li, Thomas Kirchner, George Ho, Fany Bonilla, Katharine D'Aquino, James Littrell, Rui Zhang, Wenying Jian, Xi Qiu, Songmao Zheng, Bin Gao, Peggy Wong, James N. Leonard, Raul C. Camacho   +13 more
openaire   +2 more sources

Biaryl amide glucagon receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2004
Biaryl amides derived from a reported series of ureas 1 were evaluated and found to be potent human glucagon receptor antagonists. The benzofuran analogue 6i was administered in Sprague-Dawley rats and blocked the effects of an exogenous glucagon challenge.
Ravi, Kurukulasuriya, Bryan K, Sorensen, James T, Link, Jyoti R, Patel, Hwan-Soo, Jae, Marty X, Winn, Jeffrey R, Rohde, Nelson D, Grihalde, Chun W, Lin, Christopher A, Ogiela, Andrew L, Adler, Christine A, Collins   +11 more
openaire   +2 more sources

Glucagon activates NCC in a glucagon receptor-dependent manner

Physiology, 2023
Introduction: Glucagon is raised during hypoglycemia in order to bring blood glucose back to normal levels. However, glucagon is paradoxically also raised under pathophysiological conditions where plasma glucose is high such as in diabetes mellitus (DM).
Søren Poulsen, Sara Baungaard, Laurent Bourqui, Sathish Murali, Rikke Nørregaard, Johannes Loffing, Robert Fenton   +6 more
openaire   +1 more source

Increase of glucagon receptors in hyperthyroidism

Nature, 1976
THYROID hormones influence the lipolytic response of rat adipocytes to adrenaline, glucagon, ACTH and TSH1,2. Krishna, Hynie and Brodie3 provided evidence that hyperthyroidism is followed by an increase in the nor-adrenaline-sensitive adenylate cyclase without any change in phosphodiesterase activity. Subsequent investigations have shown that adenylate
S N, Madsen, O, Sonne
openaire   +2 more sources

Regulation of Rat Glucagon Receptor Expression

Biochemical and Biophysical Research Communications, 1994
This report describes the isolation of a cDNA for the rat glucagon receptor by using the glucagon-like peptide 1 receptor cDNA as a probe. Northern blot analysis using the cDNA clone showed that the message encoding the receptor is approximately 2.3 kb in size and is expressed only in liver and kidney among seven tissues tested.
H, Yoo-Warren, A G, Willse, N, Hancock, J, Hull, M, McCaleb, J N, Livingston   +5 more
openaire   +2 more sources

Substituted Imidazoles as Glucagon Receptor Antagonists

Bioorganic & Medicinal Chemistry Letters, 2001
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC(50)=0.053 ...
L L, Chang, K L, Sidler, M A, Cascieri, S, de Laszlo, G, Koch, B, Li, M, MacCoss, N, Mantlo, S, O'Keefe, M, Pang, A, Rolando, W K, Hagmann   +11 more
openaire   +2 more sources

Characterization of the Hepatic Glucagon Receptor

Journal of Receptor Research, 1984
The hepatic glucagon receptor was covalently labeled with [125I-Tyr10]-monoiodoglucagon by use of the heterobifunctional crosslinker hydroxysuccinimidyl-p-azidobenzoate and analyzed by SDS-gel electrophoresis. The autoradiogram of the gel showed one band at Mr = 63,000 that was sensitive to excess unlabeled glucagon and GTP.
R, Iyengar, J T, Herberg, K A, Rich
openaire   +2 more sources

Potent, orally absorbed glucagon receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 1999
The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrr ole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.
S E, de Laszlo, C, Hacker, B, Li, D, Kim, M, MacCoss, N, Mantlo, J V, Pivnichny, L, Colwell, G E, Koch, M A, Cascieri, W K, Hagmann   +10 more
openaire   +2 more sources