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An orthosteric inhibitor of the Ras-Sos interaction

  作者 PATGIRI ANUPAM; YADAV KAMLESH K; ARORA PARAMJIT S; BARSAGI DAFNA  
  选自 期刊  NATURE CHEMICAL BIOLOGY;  卷期  2011年7-9;  页码  585-587  
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[摘要]Mimics of alpha-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 alpha-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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