An Orthosteric Inhibitor of the Ras-Sos Interaction

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. Herein we describe the design of a cell-permeable synthetic α-helix based on the guanine nucleotide exchange factor Sos that in...

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Detalles Bibliográficos
Autores principales: Patgiri, Anupam, Yadav, Kamlesh K., Arora, Paramjit S., Bar-Sagi, Dafna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3312813/
https://www.ncbi.nlm.nih.gov/pubmed/21765406
http://dx.doi.org/10.1038/nchembio.612
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author Patgiri, Anupam
Yadav, Kamlesh K.
Arora, Paramjit S.
Bar-Sagi, Dafna
author_facet Patgiri, Anupam
Yadav, Kamlesh K.
Arora, Paramjit S.
Bar-Sagi, Dafna
author_sort Patgiri, Anupam
collection PubMed
description 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. Herein 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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spelling pubmed-33128132012-03-26 An Orthosteric Inhibitor of the Ras-Sos Interaction Patgiri, Anupam Yadav, Kamlesh K. Arora, Paramjit S. Bar-Sagi, Dafna Nat Chem Biol Article 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. Herein 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. 2011-07-17 /pmc/articles/PMC3312813/ /pubmed/21765406 http://dx.doi.org/10.1038/nchembio.612 Text en Users may view, print, copy, download and text and data- mine the content in such documents, for the purposes of academic research, subject always to the full Conditions of use: http://www.nature.com/authors/editorial_policies/license.html#terms
spellingShingle Article
Patgiri, Anupam
Yadav, Kamlesh K.
Arora, Paramjit S.
Bar-Sagi, Dafna
An Orthosteric Inhibitor of the Ras-Sos Interaction
title An Orthosteric Inhibitor of the Ras-Sos Interaction
title_full An Orthosteric Inhibitor of the Ras-Sos Interaction
title_fullStr An Orthosteric Inhibitor of the Ras-Sos Interaction
title_full_unstemmed An Orthosteric Inhibitor of the Ras-Sos Interaction
title_short An Orthosteric Inhibitor of the Ras-Sos Interaction
title_sort orthosteric inhibitor of the ras-sos interaction
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3312813/
https://www.ncbi.nlm.nih.gov/pubmed/21765406
http://dx.doi.org/10.1038/nchembio.612
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