Drug intelligence / Profile preview

rev-erb-alpha inhibitor

Development stage
Preclinical
Lead developer
UC Davis
Modality
Small Molecules
01

Overview

Rev-erb-alpha inhibitors are a class of small molecules that target the nuclear receptor Rev-erb-alpha (NR1D1), a key component of the molecular circadian clock. While Rev-erb-alpha typically acts as a transcriptional repressor to regulate metabolism and circadian rhythms, recent research (notably from UC Davis and the Salk Institute) has identified its role in driving tumor lineage plasticity in advanced, therapy-resistant prostate cancer. By inhibiting Rev-erb-alpha, these compounds can reverse chromatin bivalency resolution, thereby suppressing the activation of neurodevelopmental and stemness programs that allow cancer cells to evade androgen receptor (AR) targeting therapies.

Other names
NR1D1 inhibitorNR-1D1 inhibitorNR 1D1 inhibitorREV-ERBA inhibitor
02

Targets

NR1D2 (Nuclear receptor subfamily 1 group D member 2)NR1D1 (Nuclear receptor subfamily 1 group D member 1)

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