Item type |
デフォルトアイテムタイプ(フル)(1) |
公開日 |
2010-02-23 |
タイトル |
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タイトル |
[総説]Rational Design to Develop Antithrombotic Drugs from the Relationship between the Structure and Function of $ \alpha $ thrombin |
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言語 |
ja |
作成者 |
Sunagawa, Masanori
Nakamura, Mariko
Shimada, Seiji
Tengan, Hiroatsu
Takara, Shigeru
Yoshioka, Miwa
Nakamura, Kazunao
Kimura, Yasutaka
Motomura, Makoto
Tamaki, Minao
Uehara, Ken
Ohta, Shigeto
Bae, Maen
Nakasone, Toshiyuki
Kosugi, Tadayoshi
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アクセス権 |
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アクセス権 |
open access |
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アクセス権URI |
http://purl.org/coar/access_right/c_abf2 |
権利情報 |
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言語 |
ja |
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権利情報 |
琉球医学会 |
主題 |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
antithrombotic drug |
主題 |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
native thrombin |
主題 |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
clot-bound thrombin |
主題 |
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言語 |
en |
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主題Scheme |
Other |
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主題 |
structure-function relationship |
内容記述 |
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内容記述タイプ |
Other |
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内容記述 |
Many protease inhibitors in the circulating blood inhibit the activity of $ \alpha $-thrombin. Inhibition of $ \alpha $-thrombin by antithrombins is attributable to the characteristics of structural relationships between $ \alpha $-thrombin and antithrombins. The characteristic structures of $ \alpha $-thrombin include loop 60, exosites 1 and 2, hydrophobic pocket, primary specificity pocket, and active site (catalytic triad). Functions of these structures have been clarified by enzyme-substrate reaction and X-ray and NMR-crystallographic analyses. For developing antithrombine drugs that is safely and effectively used for clinical treatment of thrombotic diseases, the precise understandings of relationship between structure and function of α-thrombm are required. Although it has been evidenced that clot-bound thrombm plays more important role in pathophysiological conditions than native (free) thrombin, the structure and function of clot-bound thrombin remains to be clarified. Understanding the structure and function of clot-bound thrombm would provide a potential therapeutic strategy to develop novel antithrombin drugs, which control the activity of the clot-bound thrombin in the circulating blood. In this review paper, first of all we summarized the structure-function relationships based on the studies on native thrombin and mutant thrombin. Secondary, we summarized the mechanism for thrombin receptor activation by $ \alpha $-thrombin and thrombin receptor agonist peptide (TRAP). Finally, we demonstrated our resuits of the studies on the characteristics of clot-bound thrombin |
内容記述 |
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内容記述タイプ |
Other |
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内容記述 |
論文 |
出版者 |
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言語 |
ja |
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出版者 |
琉球医学会 |
出版者 |
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言語 |
en |
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出版者 |
Ryukyu Medical Association |
言語 |
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言語 |
eng |
資源タイプ |
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資源タイプ |
journal article |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
出版タイプ |
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出版タイプ |
VoR |
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出版タイプResource |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
収録物識別子 |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
1346-888X |
収録物識別子 |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
0289-1530 |
収録物識別子 |
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収録物識別子タイプ |
NCID |
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収録物識別子 |
AN10369445 |
収録物名 |
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言語 |
ja |
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収録物名 |
琉球医学会誌 = Ryukyu Medical Journal |
書誌情報 |
巻 25,
号 3・4,
p. 95-109,
発行日 2006
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