The discovery of glucagon-like peptide-1 (GLP-1), an incretin hormone with important effects
on glycemic control and body weight regulation, led to efforts to extend its half-life and make …

G protein-coupled receptors (GPCRs) are the largest group of cell surface receptors in
humans that signal in response to diverse inputs and regulate a plethora of cellular …

Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

Tirzepatide (LY3298176) is a fatty-acid-modified, dual incretin receptor agonist that exhibits
pharmacology similar to native GIP at the glucose-dependent insulinotropic polypeptide …

INTRODUCTION Transmembrane signaling of heterotrimeric guanine nucleotide–binding
protein (G protein)–coupled receptors (GPCRs) is mediated by ligand-dependent …

Calcitonin gene-related peptide (CGRP) is a widely expressed neuropeptide that has a
major role in sensory neurotransmission. The CGRP receptor is a heterodimer of the …

Class B G-protein-coupled receptors are major targets for the treatment of chronic diseases,
including diabetes and obesity. Structures of active receptors reveal peptide agonists …

Class BG protein–coupled receptors, an important class of therapeutic targets, signal mainly
through the Gs class of heterotrimeric G proteins, although they do display some promiscuity …

G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors. Class
B1 GPCRs constitute a subfamily of 15 receptors that characteristically contain large …

G protein-coupled receptors (GPCRs) are known to interact with several other classes of
integral membrane proteins that modulate their biology and pharmacology. However, the …