マブチ　ミユキ   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	2018/01
形態種別	学術雑誌
標題	Novel Metabolically Stable PCA-1/ALKBH3 Inhibitor Has Potent Antiproliferative Effects on DU145 Cells In Vivo.
執筆形態	共著
掲載誌名	Anticancer research
掲載区分	国外
巻・号・頁	38(1),pp.211-218
著者・共著者	Ueda Masahiro, Shimizu Tadashi, Mabuchi Miyuki, Horiike Kota, Kitae Kaori, Hase Hiroaki, Ueda Yuko, Tsujikawa Kazutake, Tanaka Akito
概要	Novel potent prostate cancer antigen-1 (PCA-1)/alpha-ketoglutarate-dependent dioxygenase alkB homolog 3 (ALKBH3) inhibitors both in vivo and in vivo were designed and evaluated by a stability assay in an S9 mixture, a mixture of rat liver homogenate and co-factors, and oral absorbability assay in rat, as well as enzyme and cell assays, and resulted in the synthesis of a novel potent PCA-1/ALKBH3 inhibitor in vivo. Among them, compound 7l exhibited potent inhibitory activities in a xenograft model bearing DU145 tumor at 10 mg/kg by subcutaneous administration without negative side-effects. This inhibitory activity in vivo was more potent than that of HUHS015 at 32 mg/kg, a known PCA-1/ALKBH3 inhibitor, or docetaxel at 2.5 mg/kg, the drug clinically used for androgen-independent prostate cancer.
DOI	10.21873/anticanres.12210
ISSN	1791-7530
PMID	29277775