Synonyms: BRD4-PROTAC 12a | WWL-0245
Compound class:
Synthetic organic
Comment: WWL0245 is a bifunctional cereblon-based PROTAC molecule that promotes ubiquitin-proteasomal degradation of BRD4 protein [1]. The BET domain-binding region is based on the dual BET/PLK1 inhibitor WNY0824. Cereblon binding is mediated via a modified thalidomide moiety. WWL0245 exhibits selective cytotoxicity in BET inhibitor sensitive cancer cell lines such as androgen receptor (AR)-positive prostate cancer cell lines, and it promotes a more potent anti-proliferative effect than the parent BET inhibitor.
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References |
1. Hu R, Wang WL, Yang YY, Hu XT, Wang QW, Zuo WQ, Xu Y, Feng Q, Wang NY. (2022)
Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor. Eur J Med Chem, 227: 113922. [PMID:34700270] |