Proline-locked stapled peptides and uses thereof

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United States of America Patent

PATENT NO 9617309
SERIAL NO

14431280

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Abstract

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The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

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Patent Owner(s)

Patent OwnerAddress
PRESIDENT AND FELLOWS OF HARVARD COLLEGE17 QUINCY STREET CAMBRIDGE MA 02138

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Hayashi, Kazuhiro Cambridge, US 194 1578
Verdine, Gregory L Boston, US 123 3244

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