Clinical Importance and Potential Use of Small Molecule Inhibitors of Focal Adhesion Kinase

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Clinical Importance and Potential Use of Small Molecule Inhibitors of Focal Adhesion Kinase

Anti-Cancer Agents in Medicinal Chemistry, 11(7): 593-599.

Author(s): Alexander Schultze and Walter Fiedler.

Affiliation: University Medical Center Hamburg - Eppendorf, Hubertus Wald University Cancer Center Hamburg, Department of Oncology/Hematology with Sections BMT and Pneumology, 20246 Hamburg, Germany.


Since its first description Focal Adhesion Kinase (FAK), a cytoplasmatic tyrosine kinase, has been implicated in the formation and progression of solid and liquid malignant tumors. Therefore orally available selective small molecule inhibitors of FAK have been developed, three of them (PF-562-271, PF-04554878 and GSK2256098) are already in clinical testing. This review discusses the recent data obtained from these Phase 1 trials. We also discuss available data on the mechanisms of action of these inhibitors in carcinogenesis and demonstrate that FAK plays an important role in neoangiogenesis which is a crucial step in cancer growth.


Angiogenesis, Chemoresistance, Focal Adhesion Kinase, Metastasis, Migration of tumor cells, Small molecule inhibitors, FAK, neoangiogenesis, PF-04554878, PF-562,271.

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Article Details

Volume: 11
Issue Number: 7
First Page: 593
Last Page: 599
Page Count: 7
DOI: 10.2174/187152011796817727
Price: $58

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