Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.
Bioorg Med Chem Lett
; 21(16): 4716-9, 2011 Aug 15.
Article
en En
| MEDLINE
| ID: mdl-21764310
ABSTRACT
Described are the syntheses of three sansalvamide A derivatives that contain biotinylated tags at individual positions around the macrocycle. The tagged derivatives indicated in protein pull-down assays that they bind to Hsp90 at the same binding site (N-Middle domain) as the San A-amide peptide. Further, these compounds inhibit binding between Hsp90 and multiple C-terminal client proteins. This interaction is unique to the San A analogs indicating they can be tuned for selectivity against Hsp90 client/co-chaperone proteins.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Biotina
/
Proteínas HSP90 de Choque Térmico
/
Depsipéptidos
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2011
Tipo del documento:
Article
País de afiliación:
Estados Unidos