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

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265 Scopus citations

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
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
Externally published	Yes

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title = "An orthosteric inhibitor of the Ras-Sos interaction",

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.",

author = "Anupam Patgiri and Yadav, \{Kamlesh K.\} and Arora, \{Paramjit S.\} and Dafna Bar-Sagi",

year = "2011",

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AU - Arora, Paramjit S.

AU - Bar-Sagi, Dafna

PY - 2011/9

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N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/84860390239

U2 - 10.1038/nchembio.612

DO - 10.1038/nchembio.612

M3 - Article

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VL - 7

SP - 585

EP - 587

JO - Nature Chemical Biology

JF - Nature Chemical Biology

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An orthosteric inhibitor of the Ras-Sos interaction

Abstract

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