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Photo-leucine incorporation reveals the target of a cyclodepsipeptide inhibitor of cotranslational translocation.

Authors
  • MacKinnon, Andrew L
  • Garrison, Jennifer L
  • Hegde, Ramanujan S
  • Taunton, Jack
Type
Published Article
Journal
Journal of the American Chemical Society
Publisher
American Chemical Society
Publication Date
Nov 28, 2007
Volume
129
Issue
47
Pages
14560–14561
Identifiers
PMID: 17983236
Source
Medline
License
Unknown

Abstract

Photoaffinity labeling is a powerful tool to identify protein targets of biologically active small molecules, yet is often limited by the size, chemical properties, and availability of photoreactive groups. We report an improved synthesis of photo-leucine, a diazirine-based photoreactive analogue of leucine, and demonstrate its incorporation into a cyclodepsipeptide inhibitor of cotranslational translocation. Photoaffinity labeling in a crude membrane fraction, followed by "click chemistry" with a rhodamine-azide reporter, enabled the identification of Sec61alpha, the structural core of the Sec61 translocation channel, as the inhibitor's target.

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