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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy
Yosuke Demizu1, Keiichiro Okuhira, Hiromi Motoi
1Division of Organic Chemistry, National Institute of Health Sciences, Tokyo, Japan.
Bioorganic & Medicinal Chemistry Letters
|January 27, 2012
Abstract:
We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ERα resulting in its proteasomal degradation.
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