Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
J Med Chem
; 57(13): 5829-34, 2014 Jul 10.
Article
de En
| MEDLINE
| ID: mdl-24949551
Integrins moderate diverse important functions in the human body and are promising targets in cancer therapy. Hence, the selective inhibition of specific integrins is of great medicinal interest. Here, we report the optimization of a grafted lasso peptide, yielding MccJ25(RGDF), which is a highly potent and selective αvß3 integrin inhibitor. Furthermore, its NMR structure was elucidated and employed in a molecular dynamics approach, revealing information about the integrin binding mode and selectivity profile of MccJ25(RGDF).
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Peptides
/
Intégrine alphaVbêta3
Limites:
Humans
Langue:
En
Journal:
J Med Chem
Sujet du journal:
QUIMICA
Année:
2014
Type de document:
Article
Pays d'affiliation:
Allemagne
Pays de publication:
États-Unis d'Amérique