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タイトル: | Affinity selection and sequence-activity relationships of HIV-1 membrane fusion inhibitors directed at the drug-resistant variants |
著者: | Oishi, Shinya https://orcid.org/0000-0002-2833-2539 (unconfirmed) Watanabe, Kentaro Ito, Saori Tanaka, Michinori Nishikawa, Hiroki Ohno, Hiroaki https://orcid.org/0000-0002-3246-4809 (unconfirmed) Shimane, Kazuki Izumi, Kazuki Sakagami, Yasuko Kodama, Eiichi N. Matsuoka, Masao Asai, Akira Fujii, Nobutaka |
著者名の別形: | 大石, 真也 |
発行日: | 2010 |
出版者: | Royal Society of Chemistry |
誌名: | MedChemComm |
巻: | 1 |
号: | 4 |
開始ページ: | 276 |
終了ページ: | 281 |
抄録: | 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. |
著作権等: | © 2010 Royal Society of Chemistry 許諾条件により本文は2011-07-22に公開. 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。 This is not the published version. Please cite only the published version. |
URI: | http://hdl.handle.net/2433/126711 |
DOI(出版社版): | 10.1039/c0md00091d |
出現コレクション: | 学術雑誌掲載論文等 |
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