Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
Bioorg Med Chem Lett
; 14(13): 3457-60, 2004 Jul 05.
Article
en En
| MEDLINE
| ID: mdl-15177452
ABSTRACT
A new series of bis-statine based peptidomimetic inhibitors of human beta-secretase (BACE 1) was developed by structure-based modification of the three regions to the initial lead 3 an N-terminus, a central bis-statine core, and a C-terminus. Introduction of a 4-aminomethylbenzoic acid on the C-terminus resulted in a potent BACE 1 inhibitor with an IC50 value of 21 nM. The general requirements for the optimal substrate-enzyme interaction are disclosed herein.
Buscar en Google
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ácido Aspártico Endopeptidasas
/
Inhibidores Enzimáticos
/
Para-Aminobenzoatos
/
Aminoácidos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Estados Unidos