An orthosteric inhibitor of the Ras-Sos interaction

Anupam Patgiri; Kamlesh K. Yadav; Paramjit S. Arora; Dafna Bar-Sagi

doi:10.1038/nchembio.612

An orthosteric inhibitor of the Ras-Sos interaction

Anupam Patgiri, Kamlesh K. Yadav, Paramjit S. Arora, Dafna Bar-Sagi

Chemistry

Research output: Contribution to journal › Article › peer-review

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.

Original language	English (US)
Pages (from-to)	585-587
Number of pages	3
Journal	Nature Chemical Biology
Volume	7
Issue number	9
DOIs	https://doi.org/10.1038/nchembio.612
State	Published - Sep 2011

ASJC Scopus subject areas

Molecular Biology
Cell Biology

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10.1038/nchembio.612

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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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An orthosteric inhibitor of the Ras-Sos interaction

Abstract

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