Small-Molecule Inhibitors and Degraders Targeting KRAS-Driven Cancers.

ABSTRACT: Drug resistance continues to be a major problem associated with cancer treatment. One of the primary causes of anticancer drug resistance is the frequently mutated RAS gene. In particular, considerable efforts have been made to treat KRAS-induced cancers by directly and indirectly controlling the activity of KRAS. However, the RAS protein is still one of the most prominent targets for drugs in cancer treatment. Recently, novel targeted protein degradation (TPD) strategies, such as proteolysis-targeting chimeras, have been developed to render "undruggable" targets druggable and overcome drug resistance and mutation problems. In this study, we discuss small-molecule inhibitors, TPD-based small-molecule chemicals for targeting RAS pathway proteins, and their potential applications for treatin

SUBMITTER: Hyun S 

PROVIDER: S-EPMC8621880 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature