An Orthosteric Inhibitor of the Ras-Sos Interaction

Overview

Journal Nat Chem Biol

Specialties Biochemistry
Biology
Chemistry

Date 2011 Jul 19

PMID 21765406

Citations 133

Authors

Anupam Patgiri

Kamlesh K Yadav

Paramjit S Arora

Dafna Bar-Sagi

Affiliations

Soon will be listed here.

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.

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