Elaine Lai-Han Leung, Lian Xiang Luo, Ying Li, Zhong-Qiu Liu, Lan Lan Li, Dan Feng Shi, Ying Xie, Min Huang, Lin Lin Lu, Fu Gang Duan, Ju Min Huang, Xing Xing Fan, Zhong Wen Yuan, Jian Ding, Xiao Jun Yao, David C Ward, Liang Liu
Oncogenic KRAS is considered a promising target for anti-cancer therapy. However, direct pharmacological strategies targeting KRAS-driven cancers remained unavailable. The prenyl-binding protein PDEδ, a transporter of KRAS, has been identified as a potential target for pharmacological inhibitor by selectively binding to its prenyl-binding pocket, impairing oncogenic KRAS signaling pathway. Here, we discovered a novel PDEδ inhibitor (E)-N'-((3-(tert-butyl)-2-hydroxy-6,7,8,9-tetrahydrodibenzo[b,dfuran-1-yl)methylene)-2,4-dihydroxybenzohydrazide(NHTD) by using a high-throughput docking-based virtual screening approach...
February 20, 2019: International Journal of Cancer. Journal International du Cancer