Biologically active small molecules that interact specifically with protein have tremendous values not only for the functional analysis of genes but also for the drug development. Chemical genetics/genomics-based approach has recently been developed and recognized as one of key solutions for this purpose. This review focuses on the utilization of this new research engine for the target mining and validation of angiogenesis inhibitors that are capable of regulating the growth and spreading of cancer cells. Discovery of novel targets for angiogenesis inhibitors and validation of their biological relevancy based on chemical genetics/genomics provide new insight for the biological role of targets as well as for the development of new angiogenesis inhibitors.
Keywords: Chemical genetics/genomics, biologically active small molecules, angiogenesis inhibitors, target mining, methionine aminopeptidase 2, hsp90, histone deacetylase