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

@article{Demizu2012DesignAS,
  title={Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.},
  author={Y. Demizu and K. Okuhira and Hiromi Motoi and A. Ohno and Takuji Shoda and K. Fukuhara and H. Okuda and M. Naito and M. Kurihara},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2012},
  volume={22 4},
  pages={
          1793-6
        }
}
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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