『徳島大学 教育・研究者情報データベース (EDB)』---[学外] /
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EID=222904EID:222904, Map:0, LastModified:2013年10月3日(木) 15:37:10, Operator:[松井 栄里], Avail:TRUE, Censor:0, Owner:[宇都 義浩], Read:継承, Write:継承, Delete:継承.
種別 (必須): 学術論文 (審査論文) [継承]
言語 (必須): 英語 [継承]
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審査 (推奨): Peer Review [継承]
カテゴリ (推奨): 研究 [継承]
共著種別 (推奨):
学究種別 (推奨):
組織 (推奨):
著者 (必須): 1. (英) Kuntz A. Douglas (日) (読)
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2. (英) Nakayama Shinichi (日) (読)
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3. (英) Shea Kayla (日) (読)
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4.堀 均
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5.宇都 義浩 ([徳島大学.大学院社会産業理工学研究部.生物資源産業学域.応用生命系.応用生物資源学分野]/[徳島大学.生物資源産業学部.生物資源産業学科.応用生命講座])
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6.永澤 秀子 (岐阜薬科大学/->個人[紺世 秀子])
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7. (英) Rose R. David. (日) (読)
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題名 (必須): (英) Structural Investigation of the Binding of 5-Substituted Swainsonine Analogues to Golgi -Mannosidase II  (日)    [継承]
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要約 (任意): (英) Golgi alpha-mannosidase II (GMII) is a key enzyme in the N-glycosylation pathway and is a potential target for cancer chemotherapy. The natural product swainsonine is a potent inhibitor of GMII. In this paper we characterize the binding of 5alpha-substituted swainsonine analogues to the soluble catalytic domain of Drosophila GMII by X-ray crystallography. These inhibitors enjoy an advantage over previously reported GMII inhibitors in that they did not significantly decrease the inhibitory potential of the swainsonine head-group. The phenyl groups of these analogues occupy a portion of the binding site not previously seen to be populated with either substrate analogues or other inhibitors and they form novel hydrophobic interactions. They displace a well-organized water cluster, but the presence of a C(10) carbonyl allows the reestablishment of important hydrogen bonds. Already approximately tenfold more active against the Golgi enzyme than the lysosomal enzyme, these inhibitors offer the potential of being extended into the N-acetylglucosamine binding site of GMII for the creation of even more potent and selective GMII inhibitors.  (日)    [継承]
キーワード (推奨): 1. (英) Animals (日) (読) [継承]
2. (英) Antineoplastic Agents (日) (読) [継承]
3. (英) Binding Sites (日) (読) [継承]
4. (英) Catalytic Domain (日) (読) [継承]
5. (英) Drosophila melanogaster (日) (読) [継承]
6. (英) Golgi Apparatus (日) (読) [継承]
7. (英) Mannosidases (日) (読) [継承]
8. (英) Protein Binding (日) (読) [継承]
9. (英) Swainsonine (日) (読) [継承]
発行所 (推奨): John Wiley & Sons, Inc. [継承]
誌名 (必須): ChemBioChem ([Wiley-VCH])
(pISSN: 1439-4227, eISSN: 1439-7633)

ISSN (任意): 1439-7633
ISSN: 1439-4227 (pISSN: 1439-4227, eISSN: 1439-7633)
Title: Chembiochem : a European journal of chemical biology
Title(ISO): Chembiochem
Supplier: ChemPubSoc Europe
Publisher: Wiley Publishing
 (NLM Catalog  (Wiley  (Scopus  (CrossRef (Scopus information is found. [need login])
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(必須): 11 [継承]
(必須): 5 [継承]
(必須): 673 680 [継承]
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年月日 (必須): 西暦 2010年 3月 22日 (平成 22年 3月 22日) [継承]
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DOI (任意): 10.1002/cbic.200900750    (→Scopusで検索) [継承]
PMID (任意): 20209559    (→Scopusで検索) [継承]
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WOS (任意): 000276536000010 [継承]
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備考 (任意): 1.(英) Article.Affiliation: Ontario Cancer Institute and Department of Medical Biophysics, University of Toronto, 101 College Street, Toronto, Ontario, M5G 1L7, Canada.  (日)    [継承]
2.(英) Article.DataBankList.DataBank.DataBankName: PDB  (日)    [継承]
3.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJP  (日)    [継承]
4.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJQ  (日)    [継承]
5.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJR  (日)    [継承]
6.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJS  (日)    [継承]
7.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJT  (日)    [継承]
8.(英) Article.DataBankList.DataBank.AccessionNumberList.AccessionNumber: 3EJU  (日)    [継承]
9.(英) Article.PublicationTypeList.PublicationType: Journal Article  (日)    [継承]
10.(英) Article.PublicationTypeList.PublicationType: Research Support, N.I.H., Extramural  (日)    [継承]
11.(英) Article.PublicationTypeList.PublicationType: Research Support, Non-U.S. Gov't  (日)    [継承]
12.(英) Article.PublicationTypeList.PublicationType: Research Support, U.S. Gov't, Non-P.H.S.  (日)    [継承]

標準的な表示

和文冊子 ● Douglas A. Kuntz, Shinichi Nakayama, Kayla Shea, Hitoshi Hori, Yoshihiro Uto, Hideko Nagasawa and David. R. Rose : Structural Investigation of the Binding of 5-Substituted Swainsonine Analogues to Golgi -Mannosidase II, ChemBioChem, Vol.11, No.5, 673-680, 2010.
欧文冊子 ● Douglas A. Kuntz, Shinichi Nakayama, Kayla Shea, Hitoshi Hori, Yoshihiro Uto, Hideko Nagasawa and David. R. Rose : Structural Investigation of the Binding of 5-Substituted Swainsonine Analogues to Golgi -Mannosidase II, ChemBioChem, Vol.11, No.5, 673-680, 2010.

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