title: Focal adhesion kinase inhibitors in the treatment of metastatic cancer: a patent review.
abstract: BACKGROUND
  Focal adhesion kinase (FAK) plays a prominent role in integrin signaling. FAK activation increases phosphorylation of Tyr397 and other sites of the protein. FAK-dependent activation of signaling pathways implicated in controlling essential cellular functions including growth, proliferation, survival and migration. FERM (F for the 4.1 protein, ezrin, radixin and moesin) domain-enhanced p53 degradation plays a critical role in proliferation and survival. FAK, overexpressed in metastatic tumors, has emerged as an important therapeutic target for the development of selective inhibitors. FAK inhibitors achieved tumor growth inhibition and induced apoptosis. Strategies targeting FAK inhibition using novel compounds have created an exciting opportunity for anticancer therapy.
  
  
  METHODS
  This review summarizes the current research with available data from early phase clinical trials and discusses the available small-molecule inhibitors of FAK from patents. The importance of inhibiting FAK activity in cancer patients is discussed.
  
  
  CONCLUSIONS
  Emerging data from clinical trials with orally available small-molecule inhibitors of FAK are promising. Although this approach is appropriate as a targeted therapeutic approach against several metastatic cancer types, several compounds in research are yet to prove their preclinical efficacy. This report lays special emphasis on the available patent data of FAK inhibitors for such targeted molecular therapies. This review summarizes current knowledge about FAK inhibition in cancer therapy.
authors.affiliation: Jubilant Biosys Ltd , 96, Industrial Suburb, 2nd Stage, Yeshwanthpur, Bangalore 560 022, Karnataka , India.
authors.forename: Ekambaram
authors.initials: E
authors.lastname: Shanthi
authors.forename: Mudeenahally H
authors.initials: MH
authors.lastname: Krishna
authors.forename: Gubbi M
authors.initials: GM
authors.lastname: Arunesh
authors.forename: K
authors.initials: K
authors.lastname: Venkateswara Reddy
authors.forename: Jegatheesan
authors.initials: J
authors.lastname: Sooriya Kumar
authors.forename: Vellarkad N
authors.initials: VN
authors.lastname: Viswanadhan
mesh_terms: D002986:Clinical Trials as Topic; D051416:Focal Adhesion Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000502:physiology; D006801:Humans; D009362:Neoplasm Metastasis; D009369:Neoplasms / Q000188:drug therapy*; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D015398:Signal Transduction
chemical_list: D047428:Protein Kinase Inhibitors; D051416:Focal Adhesion Protein-Tyrosine Kinases
keywords: apoptosis; cancer; clinical trial; expression; focal adhesion kinase; growth; inhibitor; metastasis; migration; proliferation; signaling; survival