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dc.contributor.author | Oishi, Shinya | en |
dc.contributor.author | Watanabe, Kentaro | en |
dc.contributor.author | Ito, Saori | en |
dc.contributor.author | Tanaka, Michinori | en |
dc.contributor.author | Nishikawa, Hiroki | en |
dc.contributor.author | Ohno, Hiroaki | en |
dc.contributor.author | Shimane, Kazuki | en |
dc.contributor.author | Izumi, Kazuki | en |
dc.contributor.author | Sakagami, Yasuko | en |
dc.contributor.author | Kodama, Eiichi N. | en |
dc.contributor.author | Matsuoka, Masao | en |
dc.contributor.author | Asai, Akira | en |
dc.contributor.author | Fujii, Nobutaka | en |
dc.contributor.alternative | 大石, 真也 | ja |
dc.date.accessioned | 2010-10-08T00:07:33Z | - |
dc.date.available | 2010-10-08T00:07:33Z | - |
dc.date.issued | 2010 | - |
dc.identifier.issn | 2040-2503 | - |
dc.identifier.uri | http://hdl.handle.net/2433/126711 | - |
dc.description.abstract | Enfuvirtide is the first approved membrane fusion inhibitor against HIV-1. Although this drug is effective against multi-drug resistant strains, the emergence of enfuvirtide-resistant strains has been reported in patients who have received an enfuvirtide-containing regimen. Based on the high affinity of synthetic HIV-1 gp41 C-terminal heptad repeat (C-HR) peptides to the counterpart trimeric N-terminal heptad repeat (N-HR) coiled-coil structure, a novel screening approach has been established to facilitate the identification of potent fusion inhibitors against wild-type and enfuvirtide-resistant HIV-1. In this process, affinity selection using histidine-tagged N-HR peptides with the sequences derived from wild-type and resistant strains efficiently captured potent inhibitory peptides from a pool of highly water-soluble C-HR peptides with α-helix-inducible motifs. A highly potent peptide was found from a single amino acid substitution observed in an enfuvirtide-resistant variant as well as peptides with unprecedented modifications at the mutated site. | en |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | Royal Society of Chemistry | en |
dc.rights | © 2010 Royal Society of Chemistry | en |
dc.rights | 許諾条件により本文は2011-07-22に公開. | ja |
dc.rights | この論文は出版社版でありません。引用の際には出版社版をご確認ご利用ください。 | ja |
dc.rights | This is not the published version. Please cite only the published version. | en |
dc.title | Affinity selection and sequence-activity relationships of HIV-1 membrane fusion inhibitors directed at the drug-resistant variants | en |
dc.type | journal article | - |
dc.type.niitype | Journal Article | - |
dc.identifier.ncid | AA12488374 | - |
dc.identifier.jtitle | MedChemComm | en |
dc.identifier.volume | 1 | - |
dc.identifier.issue | 4 | - |
dc.identifier.spage | 276 | - |
dc.identifier.epage | 281 | - |
dc.relation.doi | 10.1039/c0md00091d | - |
dc.textversion | author | - |
dc.startdate.bitstreamsavailable | 2011-07-22 | - |
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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