Kinetics of inhibition by 5,6-dichloro-1-β-d-ribofuranosylbenzimidazole on calf thymus casein kinase II

RO Zandomeni - Biochemical Journal, 1989 - portlandpress.com
RO Zandomeni
Biochemical Journal, 1989portlandpress.com
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 …
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.
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