Completion of a Programmable DNABinding Small Molecule Library

Title:
Completion of a Programmable DNABinding Small Molecule Library
Authors:
Hsu, Carey F.; Phillips, John W.; Trauger, John W.; Farkas, Michelle E.; Belitsky, Jason M.; Heckel, Alexander; Olenyuk, Bogdan Z.; Puckett, James W.; Wang, Clay C. C.; Dervan, Peter B.
Abstract:
Hairpin pyrrole-imidazole (Py-Im) polyamides are programmable oligomers that bind the DNA minor groove in a sequence-specific manner with affinities comparable to those of natural DNA-binding proteins. These cell-permeable small molecules have been shown to enter the nuclei of live cells and downregulate endogenous gene expression. We complete here a library of 27 hairpin Py-Im polyamides, which bind seven-base-pair sequences of the general form 5′-WWGNNNW-3′ (where W=A or T, N=W, G, or C). Their equilibrium association constants (Ka) range from Ka=1×108 to 4×1010 M−1 with good sequence specificity. A table of binding affinities and sequence contexts for this completed 27-member library has been assembled for the benefit of the chemical biology community interested in molecular control of transcription.
Citation:
Hsu, C. F., J. W. Phillips, J. W. Trauger, M. E. Farkas, et al. 2007. "Completion of a Programmable DNABinding Small Molecule Library." Tetrahedron 63(27): 6146-6151.
Publisher:
Elsevier
DATE ISSUED:
2007
Department:
Chemistry
Type:
article
PUBLISHED VERSION:
10.1016/j.tet.2007.03.041
Notes:
Tetrahedron 50th Anniversary Symposium-in-Print (Part 2)
PERMANENT LINK:
http://hdl.handle.net/11282/310278

Full metadata record

DC FieldValue Language
dc.contributor.authorHsu, Carey F.en_US
dc.contributor.authorPhillips, John W.en_US
dc.contributor.authorTrauger, John W.en_US
dc.contributor.authorFarkas, Michelle E.en_US
dc.contributor.authorBelitsky, Jason M.en_US
dc.contributor.authorHeckel, Alexanderen_US
dc.contributor.authorOlenyuk, Bogdan Z.en_US
dc.contributor.authorPuckett, James W.en_US
dc.contributor.authorWang, Clay C. C.en_US
dc.contributor.authorDervan, Peter B.en_US
dc.date.accessioned2013-12-23T16:29:32Z-
dc.date.available2013-12-23T16:29:32Z-
dc.date.issued2007en
dc.identifier.citationHsu, C. F., J. W. Phillips, J. W. Trauger, M. E. Farkas, et al. 2007. "Completion of a Programmable DNABinding Small Molecule Library." Tetrahedron 63(27): 6146-6151.en_US
dc.identifier.issn0040-4020en_US
dc.identifier.urihttp://hdl.handle.net/11282/310278-
dc.description.abstractHairpin pyrrole-imidazole (Py-Im) polyamides are programmable oligomers that bind the DNA minor groove in a sequence-specific manner with affinities comparable to those of natural DNA-binding proteins. These cell-permeable small molecules have been shown to enter the nuclei of live cells and downregulate endogenous gene expression. We complete here a library of 27 hairpin Py-Im polyamides, which bind seven-base-pair sequences of the general form 5′-WWGNNNW-3′ (where W=A or T, N=W, G, or C). Their equilibrium association constants (Ka) range from Ka=1×108 to 4×1010 M−1 with good sequence specificity. A table of binding affinities and sequence contexts for this completed 27-member library has been assembled for the benefit of the chemical biology community interested in molecular control of transcription.en_US
dc.publisherElsevieren_US
dc.identifier.doi10.1016/j.tet.2007.03.041-
dc.subject.departmentChemistryen_US
dc.titleCompletion of a Programmable DNABinding Small Molecule Libraryen_US
dc.typearticleen_US
dc.description.notesTetrahedron 50th Anniversary Symposium-in-Print (Part 2)en_US
dc.identifier.journalTetrahedronen_US
dc.identifier.volume63en_US
dc.identifier.issue27en_US
dc.identifier.startpage6146en_US
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