Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.

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.

• Authors: María-Jesús Pérez-Pérez, Eva-María Priego, Ana-Isabel Hernández, María-José Camarasa, Jan Balzarini, Sandra Liekens
• Journal: Mini reviews in medicinal chemistry (Mini Rev Med Chem) Vol. 5 Issue 12 Pg. 1113-23 (Dec 2005) ISSN: 1389-5575 [Print] Netherlands
• PMID: 16375757 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

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

Topics

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