Article
A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.
Bioorganic & medicinal chemistry letters - 3 Sept 2001
Kawahata N, Yang M G, Luke G P, Shakespeare W C, Sundaramoorthi R, Wang Y, Johnson D, Merry T, Violette S, Guan W, Bartlett C, Smith J, Hatada M, Lu X, Dalgarno D C, Eyermann C J, Bohacek R S, Sawyer T K
Abstract excerpt
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...
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