title: The essential structures of ISP-I that influence serine palmitoyltransferase inhibition in Chinese hamster ovary cells.
abstract: We investigated the structure-activity relationship between various ISP-I (myriocin, thermozymocidin) analogous which has sphingosine-like structure and serine palmitoyltransferase (SPT) in Chinese hamster ovary (CHO) cells utilizing sphingolipid production as a marker. Our data suggest that the double bond and/or ketone group within the alkyl chain as well as the alkyl chain are necessary for ISP-I to inhibit SPT. In addition, a serine structure is necessary for SPT inhibitory activity, which confirms previous findings.
authors.affiliation: POLA Chemical Industries, Inc., Yokohama 224–0812, Japan. k-mizukoshi@pola.co.jp
authors.forename: Koji
authors.initials: K
authors.lastname: Mizukoshi
authors.forename: Katsuo
authors.initials: K
authors.lastname: Matsumoto
authors.forename: Ryoji
authors.initials: R
authors.lastname: Hirose
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Fujita
mesh_terms: D000818:Animals; D006224:Cricetinae; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry* / Q000494:pharmacology; D005260:Female; D010053:Ovary / Q000187:drug effects* / Q000378:metabolism; D051102:Serine C-Palmitoyltransferase / Q000037:antagonists & inhibitors*; D013107:Sphingolipids / Q000096:biosynthesis*; D013110:Sphingosine / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D005229:Fatty Acids, Monounsaturated; D013107:Sphingolipids; D051102:Serine C-Palmitoyltransferase; D013110:Sphingosine; C001996:thermozymocidin