Role of protein tyrosine kinase inhibitors in cancer therapeutics.
Protein tyrosine kinases (PTKs) are critical in regulating cell growth and differentiation and are deeply involved in several cancers. PTK-inhibitors are mainly ATP-site directed and are finding use in the treatment of several cancers, and more than 30 such agents are now in phase I-III clinical trials. The present review focuses mainly on the development of PTK inhibitors in clinical trials, with special emphasis on imatinib mesylate, a rationally designed, potent oral anticancer agent and selective inhibitor for Abl tyrosine kinase, including Bcr-Abl, C-kit and platelet-derived growth factor-receptor tyrosine kinases, which has been implicated in several malignancies, including chronic myeloid leukemia and gastrointestinal stromal tumour.
Govt. College of Pharmacy, Karad, Maharashtra 415 124, India. satishbhise@rediffmail.com
S B
SB
Bhise
Abhijit D
AD
Nalawade
Hitesh
H
Wadhawa
D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D001665:Binding Sites; D002454:Cell Differentiation; D049109:Cell Proliferation; D002986:Clinical Trials as Topic; D066246:ErbB Receptors / Q000378:metabolism; D006801:Humans; D008956:Models, Chemical; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D012008:Recurrence; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism
D000970:Antineoplastic Agents; D042461:Vascular Endothelial Growth Factor A; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases