title: Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.
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.
authors.affiliation: Division of Organic Chemistry, National Institute of Health Sciences, Tokyo, Japan.
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Demizu
authors.forename: Keiichiro
authors.initials: K
authors.lastname: Okuhira
authors.forename: Hiromi
authors.initials: H
authors.lastname: Motoi
authors.forename: Akiko
authors.initials: A
authors.lastname: Ohno
authors.forename: Takuji
authors.initials: T
authors.lastname: Shoda
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Fukuhara
authors.forename: Haruhiro
authors.initials: H
authors.lastname: Okuda
authors.forename: Mikihiko
authors.initials: M
authors.lastname: Naito
authors.forename: Masaaki
authors.initials: M
authors.lastname: Kurihara
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D001943:Breast Neoplasms; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D047628:Estrogen Receptor alpha / Q000378:metabolism; D005260:Female; D006801:Humans; D051034:Inhibitor of Apoptosis Proteins / Q000378:metabolism*; D008954:Models, Biological; D015394:Molecular Structure; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000378:metabolism*; D054875:Ubiquitination / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; C506487:ESR1 protein, human; D047628:Estrogen Receptor alpha; D051034:Inhibitor of Apoptosis Proteins; D011960:Receptors, Estrogen