Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.
Bioorg Med Chem Lett
; 19(21): 6098-101, 2009 Nov 01.
Article
em En
| MEDLINE
| ID: mdl-19800227
ABSTRACT
Previously reported structural fragments that associate with the ATP-binding pocket of basophilic protein kinases were conjugated with d-arginine-containing peptides. Inhibitory potency of the resulting bisubstrate-analog inhibitors towards PKA and ROCK-II extended to subnanomolar range. The conjugates incorporating 2-pyrimidyl-5-amidothiophene fragment had the highest activity and at 100 nM concentration exhibited over 80% inhibition of most of the tested basophilic kinases of the AGC group.
Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Adenosina
/
Proteínas Quinases Dependentes de AMP Cíclico
/
Inibidores de Proteínas Quinases
/
Quinases Associadas a rho
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2009
Tipo de documento:
Article