Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Bioorg Med Chem Lett
; 18(1): 159-63, 2008 Jan 01.
Article
en En
| MEDLINE
| ID: mdl-18036818
ABSTRACT
In an effort to obtain a MMP selective and potent inhibitor of HER-2 sheddase (ADAM-10), the P1' group of a novel class of (6S,7S)-7-[(hydroxyamino)carbonyl]-6-carboxamide-5-azaspiro[2.5]octane-5-carboxylates was attenuated and the structure-activity relationships (SAR) will be discussed. In addition, it was discovered that unconventional perturbation of the P2' moiety could confer MMP selectivity, which was hypothesized to be a manifestation of the P2' group effecting global conformational changes.
Buscar en Google
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Receptor ErbB-2
/
Inhibidores de Proteínas Quinasas
/
Proteínas ADAM
/
Secretasas de la Proteína Precursora del Amiloide
/
Ácidos Hidroxámicos
/
Proteínas de la Membrana
Tipo de estudio:
Diagnostic_studies
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2008
Tipo del documento:
Article
País de afiliación:
Estados Unidos