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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

The Molecular Mechanisms and Rational Design of Anti-Diabetic Vanadium Compounds

Author(s): Xia Niu, Ruyue Xiao, Na Wang, Ziwei Wang, Yue Zhang, Qing Xia and Xiaoda Yang

Volume 16, Issue 8, 2016

Page: [811 - 822] Pages: 12

DOI: 10.2174/1568026615666150827094652

Price: $65

Abstract

Vanadium compounds are promising anti-diabetic agents. Although BEOV was not able to succeed in phase II clinical trial, great progresses have been made in the past three decades on the discovery and development of anti-diabetic vanadium compounds. A vast of knowledge has been obtained on the molecular mechanisms of both the pharmacological and toxicological effects of vanadium complexes. It has been revealed that vanadium compounds exert insulin enhancement effects and cell protection via a multiple mechanism involving inhibition of PTP1B, activation of PPARs- AMPK signaling, regulation of unfolded protein responses (UPRs), and stimulation of antioxidant enzymes, while vanadium-induced oxidative stress and inflammatory response could primarily be attributed to vanadium toxicity. Based on the present results concerning the relationship between structures, biological activities and biochemical properties, the rationale for future design of anti-diabetic vanadium compounds has been discussed.

Keywords: Vanadium, Diabetes, Structure-activity relationship, β-cells, PTP1B, PPAR.

Graphical Abstract

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