Authors: Chyan, Yau-Jan; Chuang, Lee-Ming

Source: Recent Patents on Endocrine, Metabolic & Immune Drug Discovery, Volume 1, Number 1, February 2007 , pp. 15-24(10)

Publisher: Bentham Science Publishers

Abstract:

Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide (GLP-1) are the 2 major incretin hormones released after meals to enhance glucose-stimulated insulin secretion. In patients with type 2 diabetes, a loss of activity of GIP for insulinotropic function and a reduced secretion of GLP-1 exist in response to oral glucose while GLP-1 action is preserved. GLP-1 is therefore an attractive avenue for treating type 2 diabetes. Due to the short circulating half-life of GLP-1, which is degraded by dipeptidyl peptidase IV (DPP-IV), 2 approaches have been undertaken. One is to develop long-acting GLP-1 analogs, such as exendin-4 that is resistant to degradation. Here we review another approach for developing DPP-IV inhibitors. This group of potential drugs covers several major chemical classes and their derivatives, such as amino acid amide, carbocyclic, alkylamine, and heterocyclic compounds. More than 100 patents have been issued for DPP-IV inhibitors to be used either as a monotherapy or in combination with other antidiabetic agents for the treatment of type 2 diabetes, as well as metabolic syndrome, osteoporosis, and arthritis. Structure-based drug design is currently under intensive investigation for future development of more selective therapeutic agents.

Keywords: Dipeptidyl peptidase IV; DPP-IV inhibitors; GLP-1; type 2 diabetes

Document Type: Research article

DOI: http://dx.doi.org/10.2174/187221407779814570

Affiliations: 1: Department of Internal Medicine, National Taiwan University Hospital, 7 Chung-Shan South Road, Taipei, Taiwan.

Publication date: 2007-02-01

More about this publication?

• Recent Patents on Endocrine, Metabolic & Immune Drug Discovery publishes review articles by experts on recent patents in the field of endocrine, metabolic and immune drug discovery e.g. on novel bioactive compounds, analogs & targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in endocrine, metabolic and immune drug design and discovery.

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