A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.
Bioorg Med Chem Lett
; 11(17): 2319-23, 2001 Sep 03.
Article
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| MEDLINE
| ID: mdl-11527723
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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Base de datos:
MEDLINE
Asunto principal:
Benzamidas
/
Proteínas Proto-Oncogénicas pp60(c-src)
/
Dominios Homologos src
/
Fosfotirosina
/
Inhibidores Enzimáticos
/
Organofosfonatos
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2001
Tipo del documento:
Article
País de afiliación:
Estados Unidos