title: Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library.
abstract: Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived gamma-secretase inhibitors (GSIs). Structure-activity relationship studies indicated that (R)-configuration of alpha-substituted phenylpropanoic acid structure and cinnamic acid structure is favorable to prepare Notch-sparing GSIs.
authors.affiliation: Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Kita-ku, Okayama, Japan.
authors.forename: Motonori
authors.initials: M
authors.lastname: Kurosumi
authors.forename: Yoshino
authors.initials: Y
authors.lastname: Nishio
authors.forename: Satoko
authors.initials: S
authors.lastname: Osawa
authors.forename: Hisayoshi
authors.initials: H
authors.lastname: Kobayashi
authors.forename: Takeshi
authors.initials: T
authors.lastname: Iwatsubo
authors.forename: Taisuke
authors.initials: T
authors.lastname: Tomita
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Miyachi
mesh_terms: D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000378:metabolism*; D047495:PPAR gamma / Q000819:agonists*; D051880:Receptors, Notch / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D047495:PPAR gamma; D051880:Receptors, Notch; D053829:Amyloid Precursor Protein Secretases