Treatment of type 2 diabetes mellitus with agonists of the GLP-1 receptor or DPP-IV inhibitors.

Abstract	Glucagon-like peptide-1 (GLP-1) is a peptide hormone from the gut that stimulates insulin secretion and protects beta-cells, inhibits glucagon secretion and gastric emptying, and reduces appetite and food intake. In agreement with these actions, it has been shown to be highly effective in the treatment of Type 2 diabetes, causing marked improvements in glycaemic profile, insulin sensitivity and beta-cell performance, as well as weight reduction. The hormone is metabolised rapidly by the enzyme dipeptidyl peptidase IV (DPP-IV) and, therefore, cannot be easily used clinically. Instead, resistant analogues of the hormone (or agonists of the GLP-1 receptor) are in development, along with DPP-IV inhibitors, which have been demonstrated to protect the endogenous hormone and enhance its activity. Agonists include both albumin-bound analogues of GLP-1 and exendin-4, a lizard peptide. Clinical studies with exendin have been carried out for > 6 months and have indicated efficacy in patients inadequately treated with oral antidiabetic agents. Orally active DPP-IV inhibitors, suitable for once-daily administration, have demonstrated similar efficacy. Diabetes therapy, based on GLP-1 receptor activation, therefore, appears very promising.
Authors	Jens Juul Holst
Journal	Expert opinion on emerging drugs (Expert Opin Emerg Drugs) Vol. 9 Issue 1 Pg. 155-66 (May 2004) ISSN: 1744-7623 [Electronic] England
PMID	15155141 (Publication Type: Journal Article, Review)
Chemical References	Adenosine Deaminase Inhibitors CJC 1131 GLP1R protein, human Glp1r protein, mouse Glp1r protein, rat Glucagon-Like Peptide-1 Receptor Glycoproteins Hypoglycemic Agents Insulin Maleimides Peptide Fragments Peptides Protein Precursors Receptors, Glucagon Venoms Proglucagon Liraglutide Glucagon-Like Peptide 1 Glucagon Exenatide DPP4 protein, human Dipeptidyl Peptidase 4 Adenosine Deaminase
Topics	Adenosine Deaminase (physiology) Adenosine Deaminase Inhibitors Afferent Pathways (physiology) Animals Appetite (drug effects) Diabetes Mellitus, Experimental (drug therapy) Diabetes Mellitus, Type 2 (drug therapy, physiopathology) Dipeptidyl Peptidase 4 (physiology) Drug Therapy, Combination Exenatide Glucagon (agonists, analogs & derivatives, metabolism, pharmacology, physiology, therapeutic use) Glucagon-Like Peptide 1 Glucagon-Like Peptide-1 Receptor Glycoproteins (antagonists & inhibitors, physiology) Humans Hypoglycemic Agents (administration & dosage, pharmacology, therapeutic use) Hypothalamus (drug effects, physiopathology) Insulin (biosynthesis, genetics, metabolism) Insulin Secretion Intestinal Mucosa (innervation, metabolism) Islets of Langerhans (drug effects, metabolism) Liraglutide Lizards Maleimides (therapeutic use) Mice Mice, Knockout Mice, Obese Peptide Fragments (agonists, metabolism, pharmacology, physiology) Peptides (pharmacology, therapeutic use) Proglucagon Protein Precursors (agonists, metabolism, pharmacology, physiology) Rats Rats, Zucker Receptors, Glucagon (agonists, deficiency, physiology) Venoms (pharmacology, therapeutic use)

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