Halogenated Benzimidazoles and Benzotriazoles as Selective Inhibitors of Protein Kinases CK-I and CK-II from Saccharomyces Cerevisiae and Other Sources

Ryszard Szyszka, Nikodem Grankowski, Krzysztof Felczak, David Shugar

Research output: Contribution to journalArticlepeer-review

100 Scopus citations

Abstract

Several halogeno benzimidazole riboside inhibitors of animal and plant protein kinases CK I and CK TI (also known as casein kinases I and II), were found to be effective inhibitors of Saccharomyces cerevisiae CK II, but not of the 27-kDa CK I or the 45-kDa CK I. The previously reported 5,6-dichloro-2-azabenzimidazole, which preferentially inhibits plant CK II relative to CK I, discriminates even more effectively between the yeast CK I and CK II enzymes. Two new analogues, tetrahalogeno-2-azabenzimidazoles, are even more potent inhibitors of CK II and much less so of CK I from yeast and animal sources. All inhibitors are competitive with respect to ATP (and GTP with CK II), the two latter with Ki values in the range 0.2 - 0.6 μM for CK II from yeast and mammalian sources.

Original languageEnglish (US)
Pages (from-to)418-424
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume208
Issue number1
DOIs
StatePublished - Jan 1 1995
Externally publishedYes

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