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

作者：Demizu Yosuke; Okuhira Keiichiro; Motoi Hiromi; Ohno Akiko; Shoda Takuji; Fukuhara Kiyoshi; Okuda Haruhiro; Naito Mikihiko^*; Kurihara Masaaki

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(4): 1793-1796.

DOI：10.1016/j.bmcl.2011.11.086

• Estrogen receptor
• Protein knockdown
• Tamoxifen
• Ubiquitin-proteasome system

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.

• 出版日期2012-2-15