Cited by 237Diabetes Treatment and ManagementPeptidase Inhibition and AnalysisNatural Antidiabetic Agents Studies

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

Drucker, DJ·2003·Expert Opinion on Investigational Drugs

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.

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Crossref · 10.1517/13543784.12.1.87

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128 of 128 references verified0 citation errors · 0 not checkable

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Authors
Drucker, D.
Venue
Expert Opinion on Investigational Drugs
Published
2003-01
Volume
12
Issue
1
Pages
87-100
ISSN
  • 1354-3784 (ISSN-L)
  • 1744-7658
OpenAlex
W2112228502
Cited by
237
References
128
Citations by year
2025: 2 · 2024: 2 · 2023: 2 · 2022: 5 · 2021: 7 · 2019: 2 · 2018: 7 · 2017: 6 · 2016: 9 · 2015: 3 · 2014: 10 · 2013: 12 · 2012: 10
FWCI
4.90
Type
journal article
Language
en
Open access
closed
Locations
  • Expert Opinion on Investigational Drugs (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Health Sciences › Medicine › Oncology › Peptidase Inhibition and Analysis
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Natural Antidiabetic Agents Studies
Keywords
DPP-4 inhibitors, type 2 diabetes, incretins, glucose-dependent insulinotropic polypeptide, glucagon-like peptide-1, glucose-stimulated insulin secretion, aminopeptidase, drug development
MeSH terms
Animals, Diabetes Mellitus, Type 2, Humans, Serine Proteinase Inhibitors, Dipeptidyl Peptidase 4

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