Target intelligence / Profile preview

Gastrointestinal hormone system (GI hormone system)

Target
GI hormone system
Molecular classification
G protein-coupled receptor, Peptide hormone, Enzyme
01

Overview

The gastrointestinal hormone system is a complex network of endocrine cells and signaling peptides distributed throughout the digestive tract that coordinate digestion, nutrient absorption, and energy homeostasis [1]. Key components include hormones such as gastrin, cholecystokinin, secretin, ghrelin, and the incretins, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) [2]. These hormones primarily act through G protein-coupled receptors to regulate gastric acid secretion, gallbladder contraction, and pancreatic enzyme release [1]. Beyond local digestion, the system plays a critical role in the gut-brain-pancreas axis, influencing satiety and systemic glucose levels by modulating insulin and glucagon secretion [3]. Dysregulation of these pathways is a hallmark of metabolic diseases like type 2 diabetes and obesity, making specific receptors within the system prime therapeutic targets [2]. Modern pharmacological strategies focus on mimicking or enhancing the action of incretins or inhibiting their degradation to improve metabolic health [3].

Other names
Gut hormone systemEnteroendocrine systemDigestive endocrine systemGI endocrine system
02

Mechanism of action

Agonism of incretin receptors (GLP-1R, GIPR), inhibition of dipeptidyl peptidase-4 (DPP-4), and activation of somatostatin receptors to modulate hormone release and glucose metabolism.

03

Biological functions

Signal transductionDigestionAppetite regulationGlucose homeostasisGastric motilityAcid secretion
04

Disease associations

Diabetes mellitus type 2ObesityNeuroendocrine tumorGastroparesisZollinger-Ellison syndrome
05

Safety considerations

Gastrointestinal adverse effects (nausea, vomiting)Risk of pancreatitisPotential risk of medullary thyroid carcinomaHypoglycemia when used with secretagogues
06

Interacting drugs

5 more in the full profile.

07

Biomarkers

GastrinChromogranin AGlucagon-like peptide 1 (GLP-1)Hemoglobin A1c (HbA1c)C-peptide

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