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Development of clickable active site-directed photoaffinity probes for γ-secretase.

Abstract：

:We have developed clickable active site-directed photoaffinity probes for γ-secretase which incorporate a photoreactive benzophenone group and an alkyne handle for subsequent click chemistry mediated conjugation with azide-linked reporter tags for visualization (e.g., TAMRA-azide) or enrichment (e.g., biotin-azide) of labeled proteins. Specifically, we synthesized clickable analogs of L646 (2) and L505 (3) and validated specific labeling to presenilin-1N-terminal fragment (PS1-NTF), the active site aspartyl protease component within the γ-secretase complex. Additionally, we were able to identify signal peptide peptidase (SPP) by Western blot analysis. Furthermore, we analyzed the photo-labeled proteins in an unbiased fashion by click chemistry with TAMRA-azide followed by in-gel fluorescence detection. This approach expands the utility of γ-secretase inhibitor (GSI) photoaffinity probes in that labeled proteins can be tagged with any number of azide-linked reporters groups using a single clickable photoaffinity probe for target pull down and/or fluorescent imaging applications.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Crump CJ,am Ende CW,Ballard TE,Pozdnyakov N,Pettersson M,Chau DM,Bales KR,Li YM,Johnson DS

doi

10.1016/j.bmcl.2012.02.027

subject

Has Abstract

pub_date

2012-04-15 00:00:00

pages

2997-3000

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00219-3

journal_volume

22

pub_type

杂志文章

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