Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

By Jing Lu, Y. Qian, M. Altieri, Hanqing Dong, Jing Wang, Kanak Raina, J. Hines, J. Winkler, A. Crew, K. Coleman and 1 more. Chemistry and Biology, 2015

950 citations recorded by the source corpus.

Subfields: Hematology, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/ea46ef6a8a4664d501a843349eaad051733231c9

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In Molecular Biology

1. George M. Burslem
2. C. Crews

Citations in the corpus

• PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer (2016, background): “ARV-825 (23), a CRBN-based PROTAC with suboptimal PK, was as potent as ARV-771 in suppressing c-MYC.”
• Lessons in PROTAC design from selective degradation with a promiscuous warhead (2017, background): “Proteins effectively degraded by PROTACs include RIPK2 and ERRa (Bondeson et al., 2015), BRD4 (Lu et al., 2015; Ohoka et al., 2017; Raina et al., 2016; Winter et al., 2015), BRD9 (Remillard et al., 2017), BCR/Abl and Abl (Lai et al., 2016; Ohoka et al., 2017), and ERa (Ohoka et al., 2017).”
• Proteolysis Targeting Chimeras as Therapeutics and Tools for Biological Discovery (2020, positive): “Targeting BRD4 using PROTACs is particularly attractive since its degradation results in more robust loss of c-Myc relative to simple BRD4 inhibition, resulting in enhanced apoptosis of various cancer cells both in vitro and in vivo (Lu et al., 2015; Piya et al., 2019; Winter et al., 2015).”