Small-Molecule Gankyrin Inhibition as a Therapeutic Strategy for Breast and Lung Cancer.

ABSTRACT: Gankyrin is an oncoprotein responsible for the development of numerous cancer types. It regulates the expression levels of multiple tumor suppressor proteins (TSPs) in liver cancer; however, gankyrin's regulation of these TSPs in breast and lung cancers has not been thoroughly investigated. Additionally, no small-molecule gankyrin inhibitor has been developed which demonstrates potent anti-proliferative activity against gankyrin overexpressing breast and lung cancers. Herein, we are reporting the structure-based design of gankyrin-binding small molecules which potently inhibited the proliferation of gankyrin overexpressing A549 and MDA-MB-231 cancer cells, reduced colony formation, and inhibited the growth of 3D spheroids in an in vitro tumor simulation model. Investigations demonst

SUBMITTER: Kanabar D 

PROVIDER: S-EPMC9524259 | biostudies-literature | 2022 Jul

REPOSITORIES: biostudies-literature