Abstract
Small molecule inhibitors of multisubunit RNA polymerases (RNAP) have emerged as powerful tools for the study of transcriptional mechanisms in both prokaryotes and eukaryotes. Here, we review studies in which RNAP inhibitors such as α-amanitin, rifampicin and streptolydigin were used to reveal key molecular aspects of the transcription reaction and catalytic mechanisms of RNAP. Many of the most significant findings, that represent the main focus of this review, are related to the identification and characterization of RNAP mutants that confer resistance to inhibitors and crystallographic data of RNAP-inhibitor complexes. Understanding the mechanism of action of RNAP inhibitors may lead to the design of better drugs targeting bacterial and fungal infections as well as other human diseases such as cancer.
Keywords: Microcin J25, Streptolydigin, Rifampicin, Sorangicin A, Escherichia coli
Current Chemical Biology
Title: Inhibitors of Multisubunit RNA Polymerases as Tools to Study Transcriptional Mechanisms in Prokaryotes and Eukaryotes
Volume: 2 Issue: 1
Author(s): Benoit Coulombe, Celine Domecq, Vincent Trinh, Marie-France Langelier and Jacques Archambault
Affiliation:
Keywords: Microcin J25, Streptolydigin, Rifampicin, Sorangicin A, Escherichia coli
Abstract: Small molecule inhibitors of multisubunit RNA polymerases (RNAP) have emerged as powerful tools for the study of transcriptional mechanisms in both prokaryotes and eukaryotes. Here, we review studies in which RNAP inhibitors such as α-amanitin, rifampicin and streptolydigin were used to reveal key molecular aspects of the transcription reaction and catalytic mechanisms of RNAP. Many of the most significant findings, that represent the main focus of this review, are related to the identification and characterization of RNAP mutants that confer resistance to inhibitors and crystallographic data of RNAP-inhibitor complexes. Understanding the mechanism of action of RNAP inhibitors may lead to the design of better drugs targeting bacterial and fungal infections as well as other human diseases such as cancer.
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Coulombe Benoit, Domecq Celine, Trinh Vincent, Langelier Marie-France and Archambault Jacques, Inhibitors of Multisubunit RNA Polymerases as Tools to Study Transcriptional Mechanisms in Prokaryotes and Eukaryotes, Current Chemical Biology 2008; 2 (1) . https://dx.doi.org/10.2174/2212796810802010020
DOI https://dx.doi.org/10.2174/2212796810802010020 |
Print ISSN 2212-7968 |
Publisher Name Bentham Science Publisher |
Online ISSN 1872-3136 |
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