PMID-17928588 – The Physiology of Glucagon-Like Peptide 1

PMID-17928588 – The Physiology of Glucagon-Like Peptide 1

Holst JJ. The Physiology of Glucagon-Like Peptide 1. Physiol Rev. 2007;87(4):1409-1439.

Quick Reference

Property Value
PMID 17928588
DOI 10.1152/physrev.00034.2006
Year 2007
Journal Physiological Reviews
Study Type Narrative Review
Evidence Level V
Sample N/A (comprehensive review)
Peptide(s) Studied GLP-1 (Native)

Key Findings

  • GLP-1 is produced by post-translational processing of proglucagon in intestinal L-cells, with GLP-1(7-36) amide being the primary bioactive form
  • GLP-1 potentiates glucose-dependent insulin secretion via cAMP/PKA and Epac2 signaling pathways at the pancreatic beta-cell
  • GLP-1 suppresses glucagon secretion from alpha-cells, contributing significantly to its glucose-lowering effect
  • The peptide delays gastric emptying, which blunts postprandial glucose excursions independently of its insulinotropic action
  • DPP-4 rapidly degrades circulating GLP-1 (half-life ~2 minutes), making the native peptide impractical as a therapeutic but validating the DPP-4 inhibitor drug class
  • Central GLP-1 receptor activation in the hypothalamus and brainstem reduces appetite and food intake, establishing the basis for GLP-1RA obesity therapies

Study Design

Comprehensive narrative review synthesizing decades of GLP-1 research from the Holst laboratory and the broader field. Covers molecular biology, secretion physiology, receptor pharmacology, and organ-level effects across the pancreas, GI tract, cardiovascular system, and CNS.

Limitations

  • Published in 2007, predates the clinical development of long-acting GLP-1 receptor agonists (semaglutide, tirzepatide) and their landmark obesity/CV outcomes trials
  • Primarily integrates preclinical and early clinical data; does not address large-scale human efficacy or safety outcomes
  • Single-author review reflecting the perspective of one (albeit leading) research group

Clinical Relevance

This is the foundational reference for understanding GLP-1 physiology. It explains why GLP-1 receptor agonists work for diabetes and obesity at a mechanistic level, and why DPP-4 inhibitors were developed. Essential background for any clinician prescribing incretin-based therapies or counseling patients on GLP-1 mimetic peptides and nutraceutical approaches to enhancing endogenous GLP-1 secretion.

Related

#research #narrative-review #glp-1 #evidence-level-V