BET inhibitors in metastatic prostate cancer: therapeutic implications and rational drug combinations.

ABSTRACT:

Introduction

The bromodomain and extra-terminal (BET) family of proteins are epigenetic readers of acetylated histones regulating a vast network of protein expression across many different cancers. Therapeutic targeting of BET is an attractive area of clinical development for metastatic castration-resistant prostate cancer (mCRPC), particularly due to its putative effect on c-MYC expression and its interaction with the androgen receptor (AR). Areas covered: We speculate that a combination approach using inhibitors of BET proteins (BETi) with other targeted therapies may be required to improve the therapeutic index of BET inhibition in the management of prostate cancer. Preclinical data has identified several molecular targets that may enhance the effect of BET inhibition in the cli

SUBMITTER: Markowski MC 

PROVIDER: S-EPMC9774043 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature