title: Identification of novel SIRT2-selective inhibitors using a click chemistry approach.
abstract: A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu(I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
authors.forename: Prima R
authors.initials: PR
authors.lastname: Tatum
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Sawada
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.
authors.forename: Yosuke
authors.initials: Y
authors.lastname: Ota
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Itoh
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan.
authors.forename: Peng
authors.initials: P
authors.lastname: Zhan
authors.affiliation: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
authors.forename: Naoya
authors.initials: N
authors.lastname: Ieda
authors.affiliation: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Nakagawa
authors.affiliation: Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan. Electronic address: miyata-n@phar.nagoya-cu.ac.jp.
authors.forename: Naoki
authors.initials: N
authors.lastname: Miyata
authors.affiliation: Graduate School of Medical Science, Kyoto Prefectural University of Medicine, 13 Taishogun Nishitakatsukasa-Cho, Kita-ku, Kyoto 603-8334, Japan. Electronic address: suzukit@koto.kpu-m.ac.jp.
authors.forename: Takayoshi
authors.initials: T
authors.lastname: Suzuki
mesh_terms: D002384:Catalysis; D057930:Click Chemistry; D003300:Copper / Q000737:chemistry; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D005663:Furans / Q000737:chemistry* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology; D056565:Sirtuin 2 / Q000037:antagonists & inhibitors*; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: C000592458:A1B11SIRT2 inhibitor; C000592459:A2B57 SIRT2 inhibitor; C521855:AGK2 compound; D004791:Enzyme Inhibitors; D005663:Furans; D011804:Quinolines; D014230:Triazoles; D003300:Copper; D056565:Sirtuin 2
keywords: Histone deacetylase; Inhibitor; Isozyme selectivity; Sirtuin