Size matters, so does shape: Inhibition of transcription of T7 RNA polymerase by iron(II) clathrochelates

被引：48

作者：

Novikov, Valentin V. ^{[1
]}

Varzatskii, Oleg A. ^{[2
]}

Negrutska, Valentina V. ^{[3
]}

Bubnov, Yurii N. ^{[1
]}

Palchykovska, Larisa G. ^{[3
]}

Dubey, Igor Y. ^{[3
]}

Voloshin, Yan Z. ^{[1
]}

机构：

[1] Nesmeyanov Inst Organoelement Cpds RAS, Moscow, Russia

[2] Vernadskii Inst Gen & Inorgan Chem NASU, Kiev, Ukraine

[3] Inst Mol Biol & Genet NASU, Kiev, Ukraine

来源：

JOURNAL OF INORGANIC BIOCHEMISTRY | 2013年 / 124卷

关键词：

Drug design; Inhibitors; Clathrochelates; RNA polymerase; Macromolecular interfaces; PROTEIN-PROTEIN INTERACTIONS; IN-VITRO TRANSCRIPTION; STRUCTURAL BASIS; DIRHODIUM(II; II); COMPLEXES; ANCILLARY LIGANDS; DRUG DISCOVERY; CAGE COMPLEXES; HIV-1; PROTEASE; RUTHENIUM(II); MECHANISM;

D O I：

10.1016/j.jinorgbio.2013.03.005

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Coordination and organoelement compounds are rarely proposed as the drug candidates despite their vast potential in the area owing to their strictly controlled geometry and rather extensive surface. This is the first example of the inhibition of transcription in the system of T7 RNA polymerase by cage metal complexes. Their IC50 values reach as low as the nanomolar range, placing them among the most potent metal-based transcription inhibitors. (C) 2013 Elsevier Inc. All rights reserved.

引用

页码：42 / 45

页数：4

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