Article
Allosteric regulation of γ-secretase activity by a phenylimidazole-type γ-secretase modulator.
Proceedings of the National Academy of Sciences of the United States of America - 22 Jul 2014
Takeo Koji, Tanimura Shun, Shinoda Takehiro, Osawa Satoko, Zahariev Ivan Krasmirov, Takegami Naoki, Ishizuka-Katsura Yoshiko, Shinya Naoko, Takagi-Niidome Shizuka, Tominaga Aya, Ohsawa Noboru, Kimura-Someya Tomomi, Shirouzu Mikako, Yokoshima Satoshi, Yokoyama Shigeyuki, Fukuyama Tohru, Tomita Taisuke, Iwatsubo Takeshi
Abstract excerpt
γ-Secretase is an intramembrane-cleaving protease responsible for the generation of amyloid-β (Aβ) peptides. Recently, a series of compounds called γ-secretase modulators (GSMs) has been shown to decrease the levels of long toxic Aβ species (i.e., Aβ42), with a concomitant elevation of the produc...
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