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A Novel Phosphotyrosine Mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): Exploitation in the Design of Nonpeptide Inhibitors of Pp60(Src) SH2 Domain

Overview
Specialty Biochemistry
Date 2001 Aug 31
PMID 11527723
Citations 4
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Abstract

The novel phosphotyrosine (pTyr) mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp) has been designed and incorporated into a series of nonpeptide inhibitors of the SH2 domain of pp60(c-Src) (Src) tyrosine kinase. A 2.2 A X-ray crystal structure of 1a bound to a mutant form of Lck SH2 domain provides insight regarding the structure-activity relationships and supports the design concept of this new pTyr mimetic.

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