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Nat Chem Biol. 2011 Jul 17;7(9):585-7. doi: 10.1038/nchembio.612.

An orthosteric inhibitor of the Ras-Sos interaction.

Author information

1
Department of Chemistry, New York University, New York, New York, USA.

Abstract

Mimics of α-helices on protein surfaces have emerged as powerful reagents for antagonizing protein-protein interactions, which are difficult to target with small molecules. Here we describe the design of a cell-permeable synthetic α-helix, based on the guanine nucleotide exchange factor Sos, that interferes with Ras-Sos interaction and downregulates Ras signaling in response to receptor tyrosine kinase activation.

PMID:
21765406
PMCID:
PMC3312813
DOI:
10.1038/nchembio.612
[Indexed for MEDLINE]
Free PMC Article

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