Role of focal adhesion kinase in human cancer: a potential target for drug discovery.
The focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes to the points of cell contact with the extracellular matrix, called focal adhesions. FAK is involved in several cellular processes including invasion, motility, proliferation and apoptosis. In in vivo animal studies, FAK has been shown to contribute to tumor development and malignancy. Furthermore, FAK expression was shown to be elevated in a number of human cancers. Increased FAK expression and activity are correlated with malignant phenotype and poor prognosis in patients. Taken together, these studies suggest that FAK is a potentially good target for drug discovery. In this review, FAK and its relationship to cancer, as well as approaches to therapeutic intervention of FAK will be discussed.
Abbott Laboratories, Global Pharmaceutical Research Division, Cancer Research, 100 Abbott Park Rd, Abbott Park, IL 60064, USA. edward.k.han@abbott.com
Edward Kyu-Ho
EK
Han
Thomas
T
McGonigal
D000818:Animals; D015195:Drug Design; D051416:Focal Adhesion Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000187:drug effects; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D011743:Pyrimidines / Q000737:chemistry; D011758:Pyrroles / Q000737:chemistry; D034741:RNA, Small Interfering / Q000502:physiology
D011743:Pyrimidines; D011758:Pyrroles; C450639:Pyrrolo(2,3-d)pyrimidine; D034741:RNA, Small Interfering; D051416:Focal Adhesion Protein-Tyrosine Kinases