Abstract
Based on the X-ray structures of the pp60 Src (Src) SH2 domain complexed with two high affinity phosphopeptide ligands (Glu-Pro-Gln-pTyr-Glu-Glu-Ile-Pro-Ile-Tyr-Leu, and Ac-pTyr-Glu- D -Hcy-NH 2; Hcy = homocyclohexylalanine), we report herein the design and structure-activity relationships of a series of novel dipeptide ligands targeting the Src SH2 domain.
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