An orthosteric inhibitor of the Ras-Sos interaction

作者:Patgiri Anupam*; Yadav Kamlesh K; Arora Paramjit S; Bar Sagi Dafna
来源:Nature Chemical Biology, 2011, 7(9): 585-587.
DOI:10.1038/NCHEMBIO.612

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.

  • 出版日期2011-9