Diabetes mellitus is a chronic multifaceted disease with multiple potential complications, the
treatment of which can only delay and prolong the terminal stage of the disease, ie, type 2 …

GPCRs modulate a plethora of physiological processes and mediate the effects of one‐third
of FDA‐approved drugs. Depending on which ligand activates a receptor, it can engage …

Given the promising clinical value of allosteric modulators of G protein-coupled-receptors
(GPCRs), mechanistic understanding of how these modulators alter GPCR function is of …

G protein–coupled receptors engage both G proteins and β-arrestins, and their coupling can
be biased by ligands and mutations. Here, to resolve structural elements and mechanisms …

Summary Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone
body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for …

Cannabis use disorder (CUD) is widespread, and there is no pharmacotherapy to facilitate
its treatment. AEF0117, the first of a new pharmacological class, is a signaling-specific …

G protein-coupled receptors (GPCRs) are important drug targets that mediate various
signaling pathways by activating G proteins and engaging β-arrestin proteins. Despite its …

Allostery is a universal, biological phenomenon in which orthosteric sites are fine‐tuned by
topologically distal allosteric sites triggered by perturbations, such as ligand binding, residue …

G protein–coupled receptor (GPCR) kinases (GRKs) and arrestins interact with agonist-
bound GPCRs to promote receptor desensitization and downregulation. They also trigger …

Class BG protein-coupled receptors (GPCRs) are important targets in the treatment of
metabolic syndrome and diabetes. Although multiple structures of class B GPCRs–G protein …