Selective release of gastrointestinal hormones induced by an orally active GPR39 agonist.

ABSTRACT:

Objectives

Obesity is a complex disease associated with a high risk of comorbidities. Gastric bypass surgery, an invasive procedure with low patient eligibility, is currently the most effective intervention that achieves sustained weight loss. This beneficial effect is attributed to alterations in gut hormone signaling. An attractive alternative is to pharmacologically mimic the effects of bariatric surgery by targeting several gut hormonal axes. The G protein-coupled receptor 39 (GPR39) expressed in the gastrointestinal tract has been shown to mediate ghrelin signaling and control appetite, food intake, and energy homeostasis, but the broader effect on gut hormones is largely unknown. A potent and efficacious GPR39 agonist (Cpd1324) was recently discovered, but the in vivo functio

SUBMITTER: Grunddal KV 

PROVIDER: S-EPMC8042403 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature