PMID: 2105215Jan 12, 1990Paper

Ribofuranosyl-benzimidazole derivatives as inhibitors of casein kinase-2 and casein kinase-1

European Journal of Biochemistry
F MeggioLorenzo A Pinna

Abstract

5,6-Dichloro-1-(beta-D-ribofuranosyl)benzimidazole (DiCl-RB) is a powerful inhibitor of casein kinase-2 (CK-2) [Zandomeni, R. et al. (1986) J. Biol. Chem. 261, 3414-3420]. Here a series of 17 analogues of DiCl-RB has been employed for studying the specificity and the mode of action of this family of CK-2 inhibitors. The two halogen substituents on the benzene ring are shown to play a prominent role in inhibition, the 5,6-dibromo derivative (DiBr-RB) being fivefold more effective than DiCl-RB (Ki = 2 microM, with GTP as substrate), whereas the difluoro derivative (DiF-RB) is nearly as ineffective as unsubstituted 1-(beta-D-ribofuranosyl)benzimidazole. On the other hand, although some modifications of the ribose group significantly decrease the inhibitory efficiency, the sugar moiety is not strictly required, since dichlorobenzimidazole itself (DiCl-Bz) is an inhibitor almost as good as DiCl-RB. Inhibition of CK-2 by DiCl-RB and by its analogues, DiCl-Bz included, is of the competitive type with respect to the nucleotide substrate, the Ki values being lower with GTP than with ATP. The Ki values of the most potent inhibitor, DiBr-RB, with ATP and GTP, are 6 microM and 2 microM, respectively, denoting an affinity for the enzyme hig...Continue Reading

References

Nov 30, 1989·Biochemical and Biophysical Research Communications·K F Chan
Sep 15, 1987·European Journal of Biochemistry·F C PurvesD P Leader
Dec 15, 1987·The Biochemical Journal·P AgostinisW Merlevede
Sep 1, 1988·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·S Shenolikar
Jul 22, 1988·Proceedings of the Royal Society of London. Series B, Containing Papers of a Biological Character·P Cohen
Mar 1, 1988·European Journal of Biochemistry·A M Brunati, L A Pinna
Oct 1, 1987·Chemical & Pharmaceutical Bulletin·M HorikoshiS Natori
Dec 1, 1983·Archives of Biochemistry and Biophysics·J P TipperL A Witters
Apr 1, 1981·European Journal of Biochemistry·H BaydounK G Wagner
Aug 16, 1984·Biochemical and Biophysical Research Communications·F MeggioL A Pinna

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Citations

Jul 9, 2008·Molecular and Cellular Biochemistry·Jennifer RaafKarsten Niefind
Sep 1, 1992·The International Journal of Biochemistry·F FlamigniC M Caldarera
Sep 5, 2002·Biochemical and Biophysical Research Communications·Madalena M S BarrosoAndrea T Da Poian
Aug 23, 2002·Pharmacology & Therapeutics·Stefania SarnoLorenzo A Pinna
Aug 24, 1999·Pharmacology & Therapeutics·B GuerraL A Pinna
Aug 21, 2003·Bioorganic & Medicinal Chemistry·Mariola AndrzejewskaZygmunt Kazimierczuk
Mar 1, 1996·Nucleic Acids Research·T WadaH Handa
Mar 1, 1992·European Journal of Biochemistry·U SchubertT Porstmann
Feb 28, 2006·Journal of Virology·Peter V LidskyVadim I Agol
Jan 21, 2014·Cellular and Molecular Life Sciences : CMLS·Giorgio CozzaLorenzo A Pinna
Oct 13, 2012·Biochemical and Biophysical Research Communications·Aditi S IyengarAndrew D Hollenbach
Jan 24, 2007·The European Journal of Neuroscience·Paula G Ulery, Eric J Nestler
Jun 26, 2010·Medicinal Research Reviews·Daniel I PerezAna Martinez
Jun 16, 2009·Medicinal Research Reviews·Giorgio CozzaStefano Moro
Oct 9, 2014·European Journal of Medicinal Chemistry·I BriguglioA Carta
Jun 11, 2002·Biochemical and Biophysical Research Communications·Mário A C Silva-NetoAngela H C S Lopes
Oct 4, 2005·Biochimica Et Biophysica Acta·Stefania SarnoLorenzo A Pinna
Aug 23, 2012·Expert Opinion on Therapeutic Patents·Giorgio CozzaStefano Moro
Aug 16, 2008·Molecular BioSystems·Stefania Sarno, Lorenzo A Pinna
Mar 21, 2018·Biomedical Reports·Mathias Montenarh, Claudia Götz
Jul 1, 2008·The Biochemical Journal·Mario A PaganoLorenzo A Pinna
Apr 6, 2000·The Journal of Biological Chemistry·N MashhoonJ Kuret

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