Bioorg Med Chem Lett. 2009 Nov 1;19(21):6098-101. Epub 2009 Sep 12.

Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.

Enkvist E, Kriisa M, Roben M, Kadak G, Raidaru G, Uri A.

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Institute of Chemistry, University of Tartu, 2 Jakobi St., 51014 Tartu, Estonia.

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.

PMID:: 19800227; [PubMed - indexed for MEDLINE]

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Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.

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