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Regulation of gene expression by small molecules

Gottesfeld, Joel M. and Neely, Laura and Trauger, John T. and Baird, Eldon E. and Dervan, Peter B. (1997) Regulation of gene expression by small molecules. Nature, 387 (6629). pp. 202-205. ISSN 0028-0836. doi:10.1038/387202a0.

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Small molecules that target specific DNA sequences have the potential to control gene expression. Ligands designed for therapeutic application must bind any predetermined DNA sequence with high affinity and permeate living cells. Synthetic polyamides containing N-methylimidazole and N-methylpyrrole amino acids have an affinity and specificity for DNA comparable to naturally occurring DNA-binding proteins. We report here that an eight-ring polyamide targeted to a specific region of the transcription factor TFIIIA binding site interferes with 5S RNA gene expression in Xenopus kidney cells. Our results indicate that pyrrole-imida-zole polyamides are cell-permeable and can inhibit the transcription of specific genes.

Item Type:Article
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Dervan, Peter B.0000-0001-8852-7306
Additional Information:© 1997 Nature Publishing Group. Received 24 January; accepted 3 March 1997. We are grateful to the NIH for support of this work, the NSF for a predoctoral fellowship to J.W.T., and the Howard Hughes Medical Institute for a predoctoral fellowship to E.E.B.
Funding AgencyGrant Number
NSF Predoctoral FellowshipUNSPECIFIED
Howard Hughes Medical Institute (HHMI)UNSPECIFIED
Issue or Number:6629
Record Number:CaltechAUTHORS:20150617-103153814
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Official Citation:Regulation of gene expression by small molecules 202 Joel M. Gottesfeld, Laura Neely, John W. Trauger, Eldon E. Baird & Peter B. Dervan doi:10.1038/387202a0
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:58316
Deposited By: Ruth Sustaita
Deposited On:17 Jun 2015 18:48
Last Modified:10 Nov 2021 22:03

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