Bioorg Med Chem Lett
Institute of Chemistry, University of Tartu, 2 Jakobi St., 51014 Tartu, Estonia.
Published: November 2009
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.
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http://dx.doi.org/10.1016/j.bmcl.2009.09.026 | DOI Listing |
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