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. Author manuscript; available in PMC: 2021 Jul 9.
Published in final edited form as: J Med Chem. 2020 Jun 15;63(13):7186–7210. doi: 10.1021/acs.jmedchem.0c00456

Figure 1.

Figure 1.

BRD4 is a coregulator of ER signaling in breast cancer. (A) ER+ breast cancer is a transcriptionally driven cancer: E2-liganded ER localizes to ERE forming a transcriptional complex, including proteins such as MED1, P300, and FOXA1; BRD4 recruitment to this complex at acetylated histones and cohesin recruitment causes transcriptional elongation via P-TEFb and RNA polymerase II. Targeting the ER transcriptional complex through BRD4 provides an alternative approach either as monotherapy or in combination with SERDs to treat ER+ breast cancer. (B) Structures of benchmark BET inhibitors.