Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.
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.
Pérez-Pérez
María-Jesús
MJ
Instituto de Química Médica (CSIC), Juan de la Cierva 3, E-28006 Madrid, Spain. mjperez@iqm.csic.es
Priego
Eva-María
EM
Hernández
Ana-Isabel
AI
Camarasa
María-José
MJ
Balzarini
Jan
J
Liekens
Sandra
S
D000595:Amino Acid Sequence; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001665:Binding Sites; D015195:Drug Design; D016228:Endothelial Growth Factors / Q000502:physiology; D004730:Endothelium, Vascular / Q000166:cytology / Q000502:physiology; D004791:Enzyme Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014498:Uracil / Q000031:analogs & derivatives / Q000737:chemistry / Q000378:metabolism
D000970:Antineoplastic Agents; D016228:Endothelial Growth Factors; D004791:Enzyme Inhibitors; D014498:Uracil; C013400:6-aminouracil; D013939:Thymidine Phosphorylase