Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy

[摘要]：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 ER alpha resulting in its proteasomal degradation. (C) 2012 Published by Elsevier Ltd.

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