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dc.contributor.author | Han, Yong-Woon | en |
dc.contributor.author | Kashiwazaki, Gengo | en |
dc.contributor.author | Morinaga, Hironobu | en |
dc.contributor.author | Matsumoto, Tomoko | en |
dc.contributor.author | Hashiya, Kaori | en |
dc.contributor.author | Bando, Toshikazu | en |
dc.contributor.author | Harada, Yoshie | en |
dc.contributor.author | Sugiyama, Hiroshi | en |
dc.contributor.alternative | 韓, 龍雲 | ja |
dc.date.accessioned | 2013-09-03T00:30:12Z | - |
dc.date.available | 2013-09-03T00:30:12Z | - |
dc.date.issued | 2013-09-01 | - |
dc.identifier.issn | 0968-0896 | - |
dc.identifier.uri | http://hdl.handle.net/2433/178656 | - |
dc.description.abstract | N-Methylpyrrole (Py)-N-methylimidazole (Im) polyamides are small organic molecules that can recognize predetermined DNA sequences with high sequence specificity. As many eukaryotic promoter regions contain highly GC-rich sequences, it is valuable to synthesize and characterize Py-Im polyamides that recognize GC-rich motifs. In this study, we synthesized four hairpin Py-Im polyamides 1-4, which recognize 5'-GCGC-3' and investigated their binding behavior with surface plasmon resonance assay. Py-Im polyamides 2-4 contain two, one, and one β-alanine units, replacing the Py units of 1, respectively. The binding affinities of 2-4 to the target DNA increased 430, 390, and 610-fold, respectively, over that of 1. The association and dissociation rates of 2 to the target DNA were improved by 11 and 37-fold, respectively, compared with those of 1. Interestingly, the association and dissociation rates of 3 and 4 were higher than those of 2, even though the binding affinities of 2, 3, and 4 to the target DNA were comparable to each other. The binding affinity of 2 to DNA with a 2bp mismatch was reduced by 29-fold, compared with that to the matched DNA. Moreover, the binding affinities of 3 and 4 to the same mismatched DNA were reduced by 270 and 110-fold, respectively, indicating that 3 and 4 have greater specificities than 2 and are suitable as DNA-binding modules for engineered epigenetic regulation. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Elsevier Ltd. | en |
dc.rights | © 2013 The Authors. Published by Elsevier Ltd. | en |
dc.rights | This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. | en |
dc.subject | Pyrrole–imidazole polyamide | en |
dc.subject | Sequence specificity | en |
dc.subject | Polyamide | en |
dc.subject | DNA binding small molecule | en |
dc.title | Effect of single pyrrole replacement with β-alanine on DNA binding affinity and sequence specificity of hairpin pyrrole/imidazole polyamides targeting 5'-GCGC-3'. | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA10938083 | - |
dc.identifier.jtitle | Bioorganic & medicinal chemistry | en |
dc.identifier.volume | 21 | - |
dc.identifier.issue | 17 | - |
dc.identifier.spage | 5436 | - |
dc.identifier.epage | 5441 | - |
dc.relation.doi | 10.1016/j.bmc.2013.06.005 | - |
dc.textversion | publisher | - |
dc.identifier.pmid | 23810670 | - |
dcterms.accessRights | open access | - |
出現コレクション: | 学術雑誌掲載論文等 |
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