Patent landscape of inhibitors and PROTACs of the anti-apoptotic BCL-2 family proteins.

ABSTRACT:

Introduction

The anti-apoptotic BCL-2 family proteins, such as BCL-2, BCL-XL, and MCL-1, are excellent cancer therapeutic targets. The FDA approval of BCL-2 selective inhibitor venetoclax in 2016 validated the strategy of targeting these proteins with BH3 mimetic small molecule inhibitors.

Areas covered

This review provides an overview of the patent literature between 2016 and 2021 covering inhibitors and PROTACs of the anti-apoptotic BCL-2 proteins.

Expert opinion

Since the FDA approval of venetoclax, tremendous efforts have been made to develop its analogues with improved drug properties. These activities will likely result in new drugs in coming years. Significant progress on MCL-1 inhibitors has also been made, with multiple compounds entering clinical trials. How

SUBMITTER: Pal P 

PROVIDER: S-EPMC9942934 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature