Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372877 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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.
Graphical abstractTesting of conjugates of a series of adenosine mimics with arginine-rich peptides as inhibitors of protein kinases revealed a compound with subnanomolar inhibitory potency.Figure optionsDownload full-size imageDownload as PowerPoint slide