A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain |
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| Authors: | 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 |
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| Institution: | ARIAD Pharmaceuticals, Inc., Cambridge, MA 02139-4234, USA. |
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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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