Redox-Regulated Inhibition of T7 RNA Polymerase via Establishment of Disulfide Linkages by Substituted Dppz Dirhodium(II,II) Complexes
作者:J. Dafhne Aguirre、Helen T. Chifotides、Alfredo M. Angeles-Boza、Abdellatif Chouai、Claudia Turro、Kim R. Dunbar
DOI:10.1021/ic900164j
日期:2009.5.18
series of dirhodium(II) complexes cis-[Rh2(O2CCH3)2(R1R2dppz)2]2+1−6 (R1 = R2 = H, MeO, Me, Cl, NO2 for 1−4, 6, respectively, and R1= H, R2 = CN for 5), coordinated to R1R2dppz ligands with electron-donating or -withdrawing substituents at positions 7,8 of dppz (dppz = dipyrido[3,2-a:2′,3′-c]phenazine), were synthesized and their effect on the transcription process in vitro was monitored. Complexes 1−6 are
该系列的二铑(II)配合物的顺式- [铑2(O 2 CCH 3)2(R 1 - [R 2 dppz)2 ] 2+ 1 - 6(R 1 = R 2 = H,的MeO中,Me,氯,NO 2为1 - 4,6,分别为和R 1 = H,R 2 = CN为5),协调至R 1 - [R 2 dppz配体与供电子性或在位置吸电子取代基dppz 7,8-(dppz =双嘧啶[3,2-a: 2',3'- c ]吩嗪),并对其在体外转录过程中的作用进行了监测。配合物1 - 6容易被还原,易于氧化的半胱氨酸,并且参与与T7-RNA聚合酶(T7-RNAP),其中包含可访问的硫醇基团氧化还原反应。转录在体外通过抑制1 - 6通过形成的影响酶临界巯基半胱氨酸帧内和帧间T7-RNA聚合酶二硫键。dppz取代基(MeO