4.4 Article

A New i, i+3 Peptide Stapling System for α-Helix Stabilization

Journal

CHEMICAL BIOLOGY & DRUG DESIGN
Volume 82, Issue 6, Pages 635-642

Publisher

WILEY
DOI: 10.1111/cbdd.12231

Keywords

stapled peptides; -helix; ring-closing metathesis

Funding

  1. Johnson Johnson
  2. Harvard & Dana-Farber Program in Cancer Chemical Biology

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We have previously shown that the incorporation of an 8-atom all-hydrocarbon staple' at positions i and i+3 of a synthetic peptide results in substantial stabilization of the -helical conformation. As part of our ongoing effort to explore the scope and utility of all-hydrocarbon stapling systems, we have investigated and report herein the properties of a new i, i+3 stapling system that employs a 6-carbon cross-link.

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