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Transcription Inhibition as a Therapeutic Target for Cancer

Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Unit 1950, PO Box 301429, Houston, TX 77230-1429, USA
Author to whom correspondence should be addressed.
Cancers 2011, 3(4), 4170-4190;
Received: 18 July 2011 / Revised: 14 November 2011 / Accepted: 16 November 2011 / Published: 23 November 2011
(This article belongs to the Special Issue Cancer Diagnosis and Targeted Therapy)
PDF [542 KB, uploaded 23 November 2011]


During tumorigenesis the transformed cells lose their normal growth control mechanisms and become dependent on oncogenes’ products and pathways for survival. Treatments tailored to block the expression or function of transforming genes have shown efficacy in eliminating neoplastic cells. The mRNAs of many oncogenes, as well as regulators of other key processes such as cell proliferation, angiogenesis, and apoptosis, typically have shorter half-lives. Agents that impede mRNA synthesis are expected to selectively hinder the expression of these genes and, therefore, be detrimental to neoplastic cells that are physiologically dependent on them. In addition to exploiting the tumor cells’ dependency on short-lived transcripts, RNA-directed agents also take advantage of the differential sensitivity between transformed and non-transformed cells, as the cytotoxic effects of inhibiting RNA synthesis have not been seen in non-transformed cells. The abrogation of the formation of oncotranscripts provides a new concept in cancer therapeutics and numerous agents have been developed which are able to target transcription. The focus of this review is to give an overview of transcription and the different inhibitory strategies that target various aspects of the transcriptional process. View Full-Text
Keywords: transcription inhibitors; oncogene addiction; gene expression; ribonucleoside analogs; cyclin–dependent kinase inhibitors transcription inhibitors; oncogene addiction; gene expression; ribonucleoside analogs; cyclin–dependent kinase inhibitors
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Stellrecht, C.M.; Chen, L.S. Transcription Inhibition as a Therapeutic Target for Cancer. Cancers 2011, 3, 4170-4190.

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