マブチ　ミユキ   MIYUKI MABUCHI   馬渕　美雪    所属   兵庫医科大学  薬学部 医療薬学科    職種   助教
言語種別	英語
発行・発表の年月	2017/06
形態種別	学術雑誌
査読	査読あり
標題	Selective degradation of splicing factor CAPERα by anticancer sulfonamides.
執筆形態	共著
掲載誌名	Nature chemical biology
掲載区分	国外
巻・号・頁	13(6),pp.675-680
著者・共著者	Uehara Taisuke, Minoshima Yukinori, Sagane Koji, Sugi Naoko Hata, Mitsuhashi Kaoru Ogawa, Yamamoto Noboru, Kamiyama Hiroshi, Takahashi Kentaro, Kotake Yoshihiko, Uesugi Mai, Yokoi Akira, Inoue Atsushi, Yoshida Taku, Mabuchi Miyuki, Tanaka Akito, Owa Takashi
概要	Target-protein degradation is an emerging field in drug discovery and development. In particular, the substrate-receptor proteins of the cullin-ubiquitin ligase system play a key role in selective protein degradation, which is an essential component of the anti-myeloma activity of immunomodulatory drugs (IMiDs), such as lenalidomide. Here, we demonstrate that a series of anticancer sulfonamides NSC 719239 (E7820), indisulam, and NSC 339004 (chloroquinoxaline sulfonamide, CQS) induce proteasomal degradation of the U2AF-related splicing factor coactivator of activating protein-1 and estrogen receptors (CAPERα) via CRL4DCAF15 mediated ubiquitination in human cancer cell lines. Thus, these sulfonamides represent selective chemical probes for disrupting CAPERα function and designate DCAFs as promising drug targets for promoting selective protein degradation in cancer therapy.
DOI	10.1038/nchembio.2363
ISSN	1552-4469
PMID	28437394