Antagonizing GIPR adds fire to the GLP-1R flame

Aaron Novikoff; Timo D Müller

doi:10.1016/j.tem.2024.04.016

Antagonizing GIPR adds fire to the GLP-1R flame

Trends Endocrinol Metab. 2024 Jul;35(7):566-568. doi: 10.1016/j.tem.2024.04.016. Epub 2024 May 18.

Authors

Aaron Novikoff¹, Timo D Müller²

Affiliations

¹ Institute for Diabetes and Obesity, Helmholtz Diabetes Center, Helmholtz Munich, Neuherberg, Germany; German Center for Diabetes Research (DZD), Neuherberg, Germany.
² Institute for Diabetes and Obesity, Helmholtz Diabetes Center, Helmholtz Munich, Neuherberg, Germany; German Center for Diabetes Research (DZD), Neuherberg, Germany; Walther-Straub-Institute for Pharmacology and Toxicology, Ludwig-Maximilians-University Munich (LMU), Munich, Germany. Electronic address: timodirk.mueller@helmholtz-munich.de.

PMID: 38763780
DOI: 10.1016/j.tem.2024.04.016

Abstract

Unimolecular co-agonists at the GLP-1/GIP receptors have recently achieved remarkable anti-obesogenic feats; yet, in a recent Phase 1 clinical trial, Véniant and colleagues report astounding body-weight loss, and an appreciable safety profile, in participants with obesity using the GLP-1R agonist/GIPR antagonist AMG 133.

MeSH terms

Animals
Glucagon-Like Peptide-1 Receptor* / agonists
Glucagon-Like Peptide-1 Receptor* / metabolism
Humans
Obesity* / metabolism
Peptides / pharmacology
Receptors, Gastrointestinal Hormone* / antagonists & inhibitors
Receptors, Gastrointestinal Hormone* / metabolism
Receptors, Glucagon / antagonists & inhibitors
Receptors, Glucagon / metabolism
Weight Loss / drug effects

Substances

Glucagon-Like Peptide-1 Receptor
Receptors, Gastrointestinal Hormone
gastric inhibitory polypeptide receptor
GLP1R protein, human
Peptides
Receptors, Glucagon