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Expert Opin Investig Drugs. 2003 Jan;12(1):87-100.

Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

Author information

1
Department of Medicine, Banting and Best Diabetes Centre, Toronto General Hospital, University of Toronto, Toronto, Ontario, M5G 2C4, Canada. d.drucker@utoronto.ca

Abstract

Incretins are peptide hormones, exemplified by glucose-dependent insulinotropic peptide and glucagon-like peptide 1 that are released from the gut in response to nutrient ingestion and enhance glucose-stimulated insulin secretion. Incretin action is terminated due to N-terminal cleavage of the peptides by the aminopeptidase dipeptidyl peptidase IV (DPP-IV). Hence, inhibition of glucose-dependent insulinotropic peptide and glucagon-like peptide 1 degradation via reduction of DPP-IV activity represents an innovative strategy for enhancing incretin action in vivo. This review summarises the biology of incretin action, the structure, expression and pleiotropic biological activities of DPP-IV and provides an overview of the rationale, potential merits and theoretical pitfalls in the development of DPP-IV inhibitors for the treatment of type 2 diabetes.

PMID:
12517256
DOI:
10.1517/13543784.12.1.87
[Indexed for MEDLINE]

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