@article{oai:u-ryukyu.repo.nii.ac.jp:02015595,
 author = {Sunagawa, Masanori and Nakamura, Mariko and Shimada, Seiji and Tengan, Hiroatsu and Takara, Shigeru and Yoshioka, Miwa and Nakamura, Kazunao and Kimura, Yasutaka and Motomura, Makoto and Tamaki, Minao and Uehara, Ken and Ohta, Shigeto and Bae, Maen and Nakasone, Toshiyuki and Kosugi, Tadayoshi},
 issue = {3・4},
 journal = {琉球医学会誌 = Ryukyu Medical Journal},
 month = {},
 note = {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, 論文},
 pages = {95--109},
 title = {［総説］Rational Design to Develop Antithrombotic Drugs from the Relationship between the Structure and Function of $ \alpha $ thrombin},
 volume = {25},
 year = {2006}
}