Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
Bioorg Med Chem
; 17(8): 3053-60, 2009 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-19329328
ABSTRACT
Overexpression of zinc-dependent metalloproteinase, aminopeptidase N (APN/CD13), is considered to be involved in the process of tumor invasion and metastasis. Herein we describe the synthesis and in vitro enzymatic inhibition assay of antineoplaston AS2-5 scaffold peptidomimetic compounds. The results demonstrated that most of these L-iso-glutamine derivatives displayed selective inhibitory activity against APN as compared with MMP-2, with IC(50) values in the micromole range. The structure-activity relationships were also briefly discussed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Fenilacetatos
/
Inibidores de Proteases
/
Antígenos CD13
/
Glutamina
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article