Development of highly potent inhibitors of the Ras-targeting human acyl protein thioesterases based on substrate similarity design.
Angew Chem Int Ed Engl
; 50(42): 9832-7, 2011 Oct 10.
Article
em En
| MEDLINE
| ID: mdl-21905185
ABSTRACT
A matter of common sense a common recognition motif consisting of a negatively charged group five to six bonds away (red) from the (thio)ester functionality (green) and a positively charged tail group ten to twelve bonds away (blue) was identified in two native acyl protein thioesterase 1 (APT1) substrates. This similarity led to the design of potent inhibitors of the Ras-depalmitoylating enzyme APT1.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tioléster Hidrolases
/
Desenho de Fármacos
/
Fatores ras de Troca de Nucleotídeo Guanina
/
Inibidores Enzimáticos
/
Lactonas
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Alemanha