1.
Bioorg Med Chem Lett
; 19(21): 6098-101, 2009 Nov 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-19800227
RESUMO
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.