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.
Export Options
About this article
Cite this article as:
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
The Ambivalent Role of Apoptosis in Experimental Autoimmune Encephalomyelitis and Multiple Sclerosis
Current Pharmaceutical Design Biology of Cox-2: An Application in Cancer Therapeutics
Current Drug Targets The Nervous System as a Critical Regulator of Immune Responses Underlying Allergy
Current Pharmaceutical Design Innate Immunity in the Mucosal Immune System
Current Pharmaceutical Design Biologic Therapies in Primary Sjögren's Syndrome
Current Pharmaceutical Biotechnology CNS Immune Surveillance and Neuroinflammation: Endocannabinoids Keep Control
Current Pharmaceutical Design Targeting Class IIa HDACs: Insights from Phenotypes and Inhibitors
Current Medicinal Chemistry Epigenetics and Periodontal Disease: Hope to Tame the Untameable
Current Gene Therapy Inhibitory Effect on Replicative DNA Polymerases, Human Cancer Cell Proliferation, and In Vivo Anti-Tumor Activity by Glycolipids from Spinach
Current Medicinal Chemistry Melatonin and Respiratory Diseases: A Review
Current Topics in Medicinal Chemistry Molecular Mechanisms Involved in the Aging of the T-cell Immune Response
Current Genomics Overview of Naphthalimide Analogs as Anticancer Agents
Current Medicinal Chemistry Studies of p53 Tumor Suppression Activity in Mouse Models
Current Genomics The Role of Foxp3 in Regulatory T Cell Differentiation and Function
Current Immunology Reviews (Discontinued) Gadolinium-Deferasirox-D-Glucosamine: Novel Anti-Tumor and MR Molecular (Theranostic) Imaging Agent
Current Radiopharmaceuticals Study of the cis-trans Isomerization of the Amino-Acyl prolyl Peptide Bond. Application to the Design of Novel Inhibitors of Immunophilins
Current Organic Chemistry Immunoregulation Through 1,25-Dihydroxyvitamin D 3 and its Analogs
Current Drug Targets - Inflammation & Allergy Genetic Polymorphisms of Human Sulfate Transporters
Current Pharmacogenomics Lentiviral Vectors: A Versatile Tool to Fight Cancer
Current Molecular Medicine Anticancer Chemodiversity of Ranunculaceae Medicinal Plants: Molecular Mechanisms and Functions
Current Genomics