Comparative analysis of the substrate preferences of two post-proline cleaving endopeptidases, prolyl oligopeptidase and fibroblast activation protein α.
FEBS Lett
; 586(16): 2507-12, 2012 Jul 30.
Article
em En
| MEDLINE
| ID: mdl-22750443
ABSTRACT
Post-proline cleaving peptidases are promising therapeutic targets for neurodegenerative diseases, psychiatric conditions, metabolic disorders, and many cancers. Prolyl oligopeptidase (POP; E.C. 3.4.21.26) and fibroblast activation protein α (FAP; E.C. 3.4.24.B28) are two post-proline cleaving endopeptidases with very similar substrate specificities. Both enzymes are implicated in numerous human diseases, but their study is impeded by the lack of specific substrate probes. We interrogated a combinatorial library of proteolytic substrates and identified novel and selective substrates of POP and FAP. These new sequences will be useful as probes for fundamental biochemical study, scaffolds for inhibitor design, and triggers for controlled drug delivery.
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Serina Endopeptidases
/
Gelatinases
/
Proteínas de Membrana
Limite:
Humans
Idioma:
En
Revista:
FEBS Lett
Ano de publicação:
2012
Tipo de documento:
Article
País de afiliação:
Estados Unidos