Inhibition of Yersinia protein tyrosine phosphatase by phosphonate derivatives of calixarenes.
Bioorg Med Chem Lett
; 20(2): 483-7, 2010 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-20015646
ABSTRACT
Inhibition of Yersinia protein tyrosine phosphatase by calix[4]arene mono-, bis-, and tetrakis(methylenebisphosphonic) acids as well as calix[4]arene and thiacalix[4]arene tetrakis(methylphosphonic) acids have been investigated. The kinetic studies revealed that some compounds in this class are potent competitive inhibitors of Yersinia PTP with inhibition constants in the low micromolar range. The binding modes of macrocyclic phosphonate derivatives in the enzyme active center have been explained using computational docking approach. The results obtained indicate that calix[4]arenes are promising scaffolds for the development of inhibitors of Yersinia PTP.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Proteínas Tirosina Fosfatases
/
Calixarenos
/
Inibidores Enzimáticos
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article