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PMID: 2803263 Published · ppublish English Journal Article Research Support, U.S. Gov't, Non-P.H.S.

Kinetics of inhibition by 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole on calf thymus casein kinase II.

The Biochemical journal ·Vol. 262 ·No. 2 ·1989-09-01 ·Pages 469-73

Zandomeni RO

Abstract

The adenosine analogue 5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB) is a specific inhibitor for RNA polymerase II transcription in vivo and in vitro [Tamm + Sehgal (1978) Adv. Virus Res. 22, 187-258; Zandomeni & Weinmann (1984) J. Biol. Chem. 259, 14804-14811]. The effect on RNA polymerase II-specific transcription seems to be mediated by its inhibition of nuclear casein kinase II [Zandomeni, Carrera-Zandomeni, Shugar & Weinmann (1986) J. Biol. Chem. 261, 3414-3419]. Inhibition studies indicated that DRB acted as a mixed-type inhibitor with respect to casein and as a competitive inhibitor with respect to the nucleotide phosphate donor substrates. The DRB inhibition constant is 7 microM for the calf thymus casein kinase II, with regard to both ATP and GTP.

MeSH Terms
Animals Casein Kinases Cattle Dichlororibofuranosylbenzimidazole/pharmacology Kinetics Protein Kinase Inhibitors Ribonucleosides/pharmacology Thymus Gland/enzymology
Chemicals
Protein Kinase Inhibitors Ribonucleosides Dichlororibofuranosylbenzimidazole Casein Kinases
Authors & Affiliations
1 authors, click to expand affiliations / ORCID
Zandomeni R O
Comparative Leukemia Studies Unit, New Bolton Center, University of Pennsylvania, Kennett Square 19348.
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25 references, click to expand
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Article Info
Journal
The Biochemical journal
Abbr.
Biochem J
ISSN
0264-6021
Published
1989-09-01
Pages
469-73
Language
English
Region
England
NLM ID
2984726R
PMCID
PMC1133291
Subset
IM
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