Mapping the Binding Site of BMS-708163 on γ-Secretase with Cleavable Photoprobes

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• 作者：Natalya Gertsik¹ ; ² ; Christopher W. am Ende³ ; Kieran F. Geoghegan⁴ ; Chuong Nguyen⁴ ; Paramita Mukherjee³ ; Scot Mente⁵ ; Uthpala Seneviratne⁵ ; Douglas S. Johnson⁵ ; ^{doug.johnson@pfizer.com} ; Yue-Ming Li¹ ; ⁶ ; ⁷ ; ^{liy2@mskcc.org}
• 关键词：Alzheimer's disease ; cleavable linkers ; photoaffinity labeling ; peptide mapping ; molecular dynamics simulations
• 刊名：Cell Chemical Biology
• 出版年：2017
• 出版时间：19 January 2017
• 年：2017
• 卷：24
• 期：1
• 页码：3-8
• 全文大小：1720 K
• 卷排序：24

文摘

Developed next-generation γ-secretase inhibitor photoprobes with cleavable linkers Mapped the attachment site of a photoprobe on presenilin-1 Built a model of the structure of the γ-secretase complex with inhibitor Novel insights into the mechanism of arylsulfonamide inhibitors are provided