Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications

Mini Rev Med Chem. 2005 Dec;5(12):1113-23. doi: 10.2174/138955705774933301.

Abstract

Thymidine Phosphorylase (TPase) catalyses the reversible phosphorolysis of pyrimidine 2'-deoxynucleosides to 2-deoxyribose-1-phosphate and their respective pyrimidine bases, including the phosphorolysis of nucleoside analogues with important antiviral or anticancer properties. Moreover, TPase, identified also as the angiogenic platelet-derived endothelial cell growth factor (PD-ECGF), stimulates endothelial cell migration in vitro and angiogenesis in vivo and plays an important role in tumour progression and metastasis. Here we have summarized the most recent approaches in the search for novel TPase inhibitors together with the potential therapeutic applications of such inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Binding Sites
  • Drug Design
  • Endothelial Growth Factors / physiology
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / physiology
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Humans
  • Molecular Sequence Data
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Neoplasms / pathology
  • Thymidine Phosphorylase / antagonists & inhibitors*
  • Thymidine Phosphorylase / metabolism
  • Uracil / analogs & derivatives
  • Uracil / chemistry
  • Uracil / metabolism

Substances

  • Antineoplastic Agents
  • Endothelial Growth Factors
  • Enzyme Inhibitors
  • Uracil
  • 6-aminouracil
  • Thymidine Phosphorylase