Recognition of 16 base pairs in the minor groove of DNA by a pyrrole-imidazole polyamide dimer
Abstract
Cell-permeable small molecules that bind predetermined DNA sequences with affinities and specificities comparable to those of natural DNA-binding proteins have the potential to regulate the expression of specific genes. Recently, an eight-ring hairpin pyrrole-imidazole (Py-Im) polyamide which binds six base pairs of DNA was shown to inhibit transcription of a specific gene in cell culture. Polyamides recognizing longer DNA sequences should provide more specific biological activity. To specify a single site within the 3 billion base pair human genome, ligands which specifically recognize 15-16 base pairs are necessary. For this reason, recognition of 16 base pairs represents a milestone in the development of chemical approaches to DNA recognition. We examine here the affinity and specificity of a Py-Im polyamide dimer which targets 16 contiguous base pairs in the minor groove of DNA.
Additional Information
© 1998 American Chemical Society. Received January 5, 1998. Publication Date (Web): March 28, 1998. We are grateful to the National Institutes of Health (Grant GM-51747) for research support, to the National Science Foundation and the Ralph M. Parsons Foundation for predoctoral fellowships to J.W.T., and to the Howard Hughes Medical Institute for a predoctoral fellowship to E.E.B.Additional details
- Eprint ID
- 66862
- DOI
- 10.1021/ja9800378
- Resolver ID
- CaltechAUTHORS:20160510-093520387
- GM-51747
- NIH
- NSF Predoctoral Fellowship
- Ralph M. Parsons Foundation
- Howard Hughes Medical Institute (HHMI)
- Created
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2016-05-11Created from EPrint's datestamp field
- Updated
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2021-11-11Created from EPrint's last_modified field