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Vanadium Compounds as PTP Inhibitors

Elsa Irving1, Andrew W Stoker2

  • 1Developmental Biology and Cancer Programme, UCL Great Ormond Street Institute of Child Health, 30 Guilford Street, London WC1N 1EH, UK. elsa.irving.15@ucl.ac.uk.

Molecules (Basel, Switzerland)
|December 20, 2017
PubMed

Insights

Vanadium compounds show potential as protein tyrosine phosphatase (PTP) inhibitors for treating diabetes and cancer. Further research is needed to improve their delivery and reduce toxicity for therapeutic use.

Area of Science:

  • Biochemistry
  • Medicinal Chemistry
  • Pharmacology

Background:

  • Phosphotyrosine signaling is crucial, regulated by protein tyrosine kinases (PTKs) and phosphatases (PTPs).
  • Vanadium derivatives are explored as potential inhibitors of PTPs and as metallotherapeutics.

Purpose of the Study:

  • To review the potential of vanadium derivatives as PTP inhibitors and metallotherapeutics.
  • To discuss recent developments in the biological and biochemical actions of complex vanadium compounds.
  • To examine pre-clinical anti-diabetic and anti-cancer studies.

Main Methods:

  • Review of literature on vanadium compounds, PTP inhibition, and pre-clinical studies.
  • Discussion of the mechanisms of PTP inhibition by vanadate and its derivatives.
  • Analysis of biological and biochemical effects of complex vanadium compounds.

Main Results:

  • Vanadate (V oxidized state) acts as a pan-inhibitor of PTPs.
  • Complex vanadium derivatives, including decavanadate and oxidovanadium compounds with organic ligands, show pre-clinical efficacy in anti-diabetic and anti-cancer contexts.
  • PTP inhibition is implicated, but other biochemical effects and off-target toxicities are observed.

Conclusions:

  • Vanadium compounds hold therapeutic promise, but clinical trial progress is hindered by toxicity concerns.
  • Improved delivery and tissue targeting are crucial to minimize off-target toxicities and realize the full therapeutic potential of vanadium compounds.
  • Continued interest in vanadium-based metallotherapeutics persists despite current challenges.
Keywords:
BMOVPTPcancerdiabetesoxidovanadiumoxovanadiumprotein tyrosine phosphatasesvanadatevanadium

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