title: Synthesis of biotinylated photoaffinity probes based on arylsulfonamide gamma-secretase inhibitors.
abstract: Synthesis and biological evaluation of an arylsulfonamide class of gamma-secretase inhibitors are described. Design, synthesis, and biological evaluation of multifunctional molecular probes harboring a benzophenone photophore as a cross-linking group and a biotin tag are also reported.
authors.affiliation: Graduate School of Pharmaceutical Sciences, University of Tokyo, Bunkyo-ku, Japan. hfuwa@bios.tohoku.ac.jp
authors.forename: Haruhiko
authors.initials: H
authors.lastname: Fuwa
authors.forename: Kenichi
authors.initials: K
authors.lastname: Hiromoto
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Takahashi
authors.forename: Satoshi
authors.initials: S
authors.lastname: Yokoshima
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Kan
authors.forename: Tohru
authors.initials: T
authors.lastname: Fukuyama
authors.forename: Takeshi
authors.initials: T
authors.lastname: Iwatsubo
authors.forename: Taisuke
authors.initials: T
authors.lastname: Tomita
authors.forename: Hideaki
authors.initials: H
authors.lastname: Natsugari
mesh_terms: D053829:Amyloid Precursor Protein Secretases; D001190:Arylsulfonates / Q000737:chemistry*; D019921:Biotinylation; D002087:Butyrates / Q000494:pharmacology; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003432:Cross-Linking Reagents / Q000494:pharmacology; D015195:Drug Design; D010450:Endopeptidases / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006846:Hydrocarbons, Halogenated / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008027:Light; D008956:Models, Chemical; D019920:Photoaffinity Labels / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: C497115:4-(2-((1R)-1-(((4-chlorophenyl)sulfonyl)-2,5-difluoroanilino)ethyl)-5-fluorophenyl)butanoic acid; D001190:Arylsulfonates; D002087:Butyrates; D003432:Cross-Linking Reagents; D004791:Enzyme Inhibitors; D006846:Hydrocarbons, Halogenated; D019920:Photoaffinity Labels; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases