Dysregulation of the basal RNA polymerase transcription apparatus in cancer.

Abstract

Mutations that directly affect transcription by RNA polymerases rank among the most central mediators of malignant transformation, but the frequency of new anticancer drugs that selectively target defective transcription apparatus entering the clinic has been limited. This is because targeting the large protein-protein and protein-DNA interfaces that control both generic and selective aspects of RNA polymerase transcription has proved extremely difficult. However, recent technological advances have led to a 'quantum leap' in our comprehension of the structure and function of the core RNA polymerase components, how they are dysregulated in a broad range of cancers and how they may be targeted for 'transcription therapy'.

• Authors: Megan J Bywater, Richard B Pearson, Grant A McArthur, Ross D Hannan
• Journal: Nature reviews. Cancer (Nat Rev Cancer) Vol. 13 Issue 5 Pg. 299-314 (May 2013) ISSN: 1474-1768 [Electronic] England
• PMID: 23612459 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Antineoplastic Agents
• Transcription Factors, General
• DNA-Directed RNA Polymerases

Topics

• Animals
• Antineoplastic Agents (pharmacology)
• Cell Transformation, Neoplastic (genetics, metabolism)
• DNA-Directed RNA Polymerases (physiology)
• Gene Expression Regulation, Neoplastic
• Humans
• Molecular Targeted Therapy
• Mutation
• Neoplasms (drug therapy, enzymology, genetics)
• Oncogenes
• Transcription Factors, General (genetics, metabolism)
• Transcriptional Activation (drug effects)