Zandomeni R O
Comparative Leukemia Studies Unit, New Bolton Center, University of Pennsylvania, Kennett Square 19348.
Biochem J. 1989 Sep 1;262(2):469-73. doi: 10.1042/bj2620469.
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.
腺苷类似物5,6-二氯-1-β-D-呋喃核糖基苯并咪唑(DRB)是体内和体外RNA聚合酶II转录的特异性抑制剂[Tamm + Sehgal(1978年)《病毒研究进展》22,187 - 258;Zandomeni & Weinmann(1984年)《生物化学杂志》259,14804 - 14811]。对RNA聚合酶II特异性转录的影响似乎是通过其对核酪蛋白激酶II的抑制作用介导的[Zandomeni,Carrera - Zandomeni,Shugar & Weinmann(1986年)《生物化学杂志》261,3414 - 3419]。抑制研究表明,DRB对酪蛋白而言是混合型抑制剂,对核苷酸磷酸供体底物而言是竞争性抑制剂。就ATP和GTP而言,小牛胸腺酪蛋白激酶II的DRB抑制常数为7微摩尔。