Peptide-assisted enhancement of inhibitory effects of small molecular inhibitors for kinases

Authors: Wang, Wei; Hirano, Yoshinori; Uzawa, Takanori; Taiji, Makoto; Ito, Yoshihiro; Bulletin of the Chemical Society of Japan; (2016); 10.1246/bcsj.20150414

Conjugation of small molecular inhibitor with a site recognition peptide would generate highly potent peptide–drug conjugate inhibitors of protein kinases. A peptide selected by ribosome display with a tRNA carrying an inhibitor-conjugated amino acid exhibited up to 10- to 100-fold higher inhibitory effects towards different kinases than solely the inhibitor