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Protein Kinases and Phosphatases02:54

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Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
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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
Summary
This summary is machine-generated.

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.

Keywords:
BMOVPTPcancerdiabetesoxidovanadiumoxovanadiumprotein tyrosine phosphatasesvanadatevanadium

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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.