| ○種別 (必須): |
| ○言語 (必須): | □ | 英語
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| ○カテゴリ (推奨): |
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| ○学究種別 (推奨): |
| ○組織 (推奨): |
| ○著者 (必須): | 1. | (英) Davison R. Holly (日) (読)
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| 2. | (英) Taylor Stephanie (日) (読)
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| 3. | (英) Drake Chris (日) (読)
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| 4. | (英) Phuan Puay-Wah (日) (読)
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| 5. | (英) Derichs Nico (日) (読)
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| 6. | 姚 陳娟 ([徳島大学.大学院医歯薬学研究部.歯学域.口腔科学部門.基礎歯学系.口腔生理学])
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| 7. | (英) Jones F. Ella (日) (読)
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| 8. | (英) Sutcliffe Julie (日) (読)
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| 9. | (英) Verkman S. A (日) (読)
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| 10. | (英) Kurth J. Mark (日) (読)
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| ○題名 (必須): | □ | (英) Functional fluorescently labeled bithiazole ΔF508-CFTR corrector imaged in whole body slices in mice. (日)
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| ○要約 (任意): | □ | (英) We previously reported the identification and structure-activity analysis of bithiazole-based correctors of defective cellular processing of the cystic fibrosis-causing CFTR mutant, ΔF508-CFTR. Here, we report the synthesis and uptake of a functional, fluorescently labeled bithiazole corrector. Following synthesis and functional analysis of four bithiazole-fluorophore conjugates, we found that 5, a bithazole-based BODIPY conjugate, had low micromolar potency for correction of defective ΔF508-CFTR cellular misprocessing, with comparable efficacy to benchmark corrector corr-4a. Intravenous administration of 5 to mice established its stability in extrahepatic tissues for tens of minutes. By fluorescence imaging of whole-body frozen slices, fluorescent corrector 5 was visualized strongly in gastrointestinal organs, with less in lung and liver. Our results provide proof-of-concept for mapping the biodistribution of a ΔF508-CFTR corrector by fluorophore labeling and fluorescence imaging of whole-body slices. (日)
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| ○キーワード (推奨): | 1. | (英) Animals (日) (読)
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| 2. | (英) Boron Compounds (日) (読)
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| 3. | (英) Cystic Fibrosis (日) (読)
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| 4. | (英) Cystic Fibrosis Transmembrane Conductance Regulator (日) (読)
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| 5. | (英) Fluorescent Dyes (日) (読)
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| 6. | (英) Mice (日) (読)
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| 7. | (英) Mutation (日) (読)
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| 8. | (英) Thiazoles (日) (読)
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| 9. | (英) Whole Body Imaging (日) (読)
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| ○発行所 (推奨): |
| ○誌名 (必須): | □ | Bioconjugate Chemistry ([アメリカ化学会])
(pISSN: 1043-1802, eISSN: 1520-4812)
| ○ISSN (任意): | □ | 1520-4812
ISSN: 1043-1802
(pISSN: 1043-1802, eISSN: 1520-4812) Title: Bioconjugate chemistryTitle(ISO): Bioconjug ChemPublisher: American Chemical Society (NLM Catalog)
(Scopus)
(CrossRef)
(Scopus information is found. [need login]) | [継承] |
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| ○巻 (必須): | □ | 22
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| ○号 (必須): | □ | 12
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| ○頁 (必須): | □ | 2593 2599
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| ○都市 (任意): |
| ○年月日 (必須): | □ | 西暦 2011年 11月 18日 (平成 23年 11月 18日)
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| ○URL (任意): |
| ○DOI (任意): | □ | 10.1021/bc2004457 (→Scopusで検索)
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| ○PMID (任意): | □ | 22034937 (→Scopusで検索)
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| ○備考 (任意): | 1. | (英) Article.Affiliation: Department of Chemistry, University of California, Davis, Davis, California 95616, United States. (日)
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| 2. | (英) Article.PublicationTypeList.PublicationType: Journal Article (日)
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| 3. | (英) Article.PublicationTypeList.PublicationType: Research Support, N.I.H., Extramural (日)
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| 4. | (英) Article.PublicationTypeList.PublicationType: Research Support, Non-U.S. Gov't (日)
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| 5. | (英) Article.PublicationTypeList.PublicationType: Research Support, U.S. Gov't, Non-P.H.S. (日)
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| 6. | (英) OtherID: NIHMS339902 [Available on 12/21/12] (日)
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| 7. | (英) OtherID: PMC3245868 [Available on 12/21/12] (日)
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