Clinical importance and potential use of small molecule inhibitors of focal adhesion kinase.
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Clinical importance and potential use of small molecule inhibitors of focal adhesion kinase. / Schultze, Alexander; Fiedler, Walter.
In: ANTI-CANCER AGENT ME, Vol. 11, No. 7, 7, 2011, p. 593-599.Research output: SCORING: Contribution to journal › SCORING: Journal article › Research › peer-review
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TY - JOUR
T1 - Clinical importance and potential use of small molecule inhibitors of focal adhesion kinase.
AU - Schultze, Alexander
AU - Fiedler, Walter
PY - 2011
Y1 - 2011
N2 - 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.
AB - 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.
M3 - SCORING: Journal article
VL - 11
SP - 593
EP - 599
JO - ANTI-CANCER AGENT ME
JF - ANTI-CANCER AGENT ME
SN - 1871-5206
IS - 7
M1 - 7
ER -