A 4-week study assessing the pharmacokinetics, pharmacodynamics, safety, and tolerability of the glucagon receptor antagonist PF-06291874 administered as monotherapy in subjects with type 2 diabetes mellitus.
Sign Up to like & getrecommendations! Published in 2017 at "Diabetes research and clinical practice"
DOI: 10.1016/j.diabres.2017.01.019
Abstract: AIMS The glucagon receptor antagonist PF-06291874 has demonstrated robust glucose reductions in subjects with type 2 diabetes mellitus (T2DM) on background metformin. This study assessed the pharmacokinetics, pharmacodynamics, safety, and tolerability of PF-06291874 administered as… read more here.
Keywords: receptor antagonist; monotherapy; safety; glucagon receptor ... See more keywords
Antagonistic Effect and In Vitro Activity of Dauricine on Glucagon Receptor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of natural products"
DOI: 10.1021/acs.jnatprod.2c00446
Abstract: Abnormal increases in glucagon (GCG) are the primary cause of type II diabetes mellitus. When GCG interacts with a glucagon receptor (GCGR), GCG can increase the blood glucose level. In this paper, a compound that… read more here.
Keywords: receptor; antagonistic effect; dauricine; glucagon receptor ... See more keywords
Stapled, Long-Acting Xenopus GLP-1-Based Dual GLP-1/Glucagon Receptor Agonists with Potent Therapeutic Efficacy for Metabolic Disease.
Sign Up to like & getrecommendations! Published in 2021 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.0c00995
Abstract: Novel peptidic glucagon receptor (GCGR) and glucagon-like peptide 1 receptor (GLP-1R) dual agonists are reported to have increased efficacy over GLP-1R monoagonists for the treatment of diabetes and obesity. We identified a novel Xenopus GLP-1-based… read more here.
Keywords: xenopus glp; glp based; glp; glucagon receptor ... See more keywords
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00217
Abstract: Peptide-based analogues of the gut-derived incretin hormone, glucagon-like peptide 1 (GLP1), stimulate insulin secretion in a glucose-dependent manner. Currently marketed GLP1 receptor (GLP1R) agonists are safe and effective in the management of Type 2 diabetes… read more here.
Keywords: dual agonist; chemistry; glucagon; glucagon receptor ... See more keywords
A combined activation mechanism for the glucagon receptor
Sign Up to like & getrecommendations! Published in 2020 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.1921851117
Abstract: Significance Understanding the mechanisms of activation of G-protein–coupled receptors (GPCRs) is a major issue in biophysics and pharmacology. This is particularly true for peptide-activated class B receptors, which are more flexible and have been studied… read more here.
Keywords: receptor; activation mechanism; glucagon receptor; activation ... See more keywords
Investigational glucagon receptor antagonists in Phase I and II clinical trials for diabetes
Sign Up to like & getrecommendations! Published in 2017 at "Expert Opinion on Investigational Drugs"
DOI: 10.1080/13543784.2017.1395020
Abstract: ABSTRACT Introduction: Despite type 2 diabetes (T2D) being recognized as a bihormonal pancreatic disease, current therapies are mainly focusing on insulin, while targeting glucagon has been long dismissed. However, glucagon receptor (GCGr) antagonists are currently… read more here.
Keywords: gcgr antagonists; antagonists phase; glucagon receptor; clinical trials ... See more keywords
Negative allosteric modulation of the glucagon receptor by RAMP2
Sign Up to like & getrecommendations! Published in 2022 at "Cell"
DOI: 10.1101/2022.08.30.505955
Abstract: Receptor activity-modifying proteins (RAMPs) modulate the activity of many Family B heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs). The glucagon receptor (GCGR), a Family B GPCR responsible for maintenance of proper blood sugar levels,… read more here.
Keywords: gcgr; ramp2; receptor; negative allosteric ... See more keywords
MEDI0382, a GLP‐1/glucagon receptor dual agonist, meets safety and tolerability endpoints in a single‐dose, healthy‐subject, randomized, Phase 1 study
Sign Up to like & getrecommendations! Published in 2018 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.13688
Abstract: MEDI0382 is a balanced glucagon‐like peptide‐1/glucagon receptor dual agonist under development for the treatment of type 2 diabetes mellitus and non‐alcoholic steatohepatitis. The primary objective was to assess the safety of MEDI0382 in healthy subjects. read more here.
Keywords: glucagon receptor; receptor dual; dual agonist;
A randomized Phase I study of the safety, tolerability, pharmacokinetics and pharmacodynamics of BI 456906, a dual glucagon receptor/glucagon‐like peptide‐1 receptor agonist, in healthy Japanese men with overweight/obesity
Sign Up to like & getrecommendations! Published in 2023 at "Diabetes"
DOI: 10.1111/dom.15064
Abstract: To report a Phase I study of subcutaneous glucagon receptor (GCGR)/glucagon‐like peptide‐1 receptor (GLP‐1R) dual agonist BI 456906 versus placebo in healthy Japanese men with overweight/obesity. read more here.
Keywords: glucagon like; glucagon; phase study; like peptide ... See more keywords
RAMP2 Influences Glucagon Receptor Pharmacology via Trafficking and Signaling
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DOI: 10.1210/en.2016-1755
Abstract: Endogenous satiety hormones provide an attractive target for obesity drugs. Glucagon causes weight loss by reducing food intake and increasing energy expenditure. To further understand the cellular mechanisms by which glucagon and related ligands activate… read more here.
Keywords: gcgr; microscopy; ramp2; glucagon receptor ... See more keywords
Increased SLC38A4 Amino Acid Transporter Expression in Human Pancreatic &agr;-Cells After Glucagon Receptor Inhibition
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DOI: 10.1210/en.2019-00022
Abstract: Plasma amino acids and their transporters constitute an important part of the feedback loop between the liver and pancreatic α-cell function, and glucagon regulates hepatic amino acid turnover. Disruption of hepatic glucagon receptor action activates… read more here.
Keywords: amino; amino acid; glucagon receptor; expression ... See more keywords