c-MET kinase inhibitors: a patent review (2011 - 2013).

摘要: Introduction: The receptor tyrosine kinase c-MET displays aberrant activation in the malignant phenotype of various tumors, and thus, has drawn considerable attention as drug target for cancer therapy. Many inhibitors are now under clinical investment, one them – Cabozantinib been approved by US FDA 2012 treatment medullary thyroid cancer, which further proved feasibility inhibition method Areas covered: This article briefly outlines role oncogenesis provides a broad overview assays used to characterize new inhibitors. Then, series representative small-molecule c-MET, especially from published patent literature 2011 2013, recorded. Herein, challenges inhibitor design, such selectivity resistance mutations, also discussed. Expert opinion: Up now, at least 17 evaluation, several agents exhibit e...