Title:
ANTICOAGULANT POLYPEPTIDES AND USES THEREOF
Document Type and Number:
WIPO Patent Application WO/2010/054503
Kind Code:
A1
Abstract:
The present invention discloses the anticoagulant polypeptides, which have the following primary structure formula: (D)-FPRP-X1-X2-X3-X4-X5-QGDFEPIPEDAYDE-NH2; wherein X1 selected from any one of G, AEEA, K and R; X2 selected from any one of G, K and R, or X2 deleted; X3 selected from any one of G, K and D, or X3 deleted; X4 selected from any one of G, K, W and D; X5 selected from any one of P and S, or X5 deleted; wherein K is lysine modified with fatty acid, said fatty acid in particular is stearic acid. According to the structures of thrombin and anticoagulant medicine Bivalirudin and interaction thereof, a class of polypeptides are designed and synthesized in the present invention. The anticoagulant polypeptides of the present invention not only can inhibit the activity of thrombin effectively and specifically, but also have similar amount of amino acids to Bivalirudin. The anticoagulant polypeptides can be synthesized easily and have high anticoagulant activity.
Inventors:
DAI QIUYUN (CN)
HUANG YUANYUAN (CN)
DONG MINGXIN (CN)
YU ZHENG (CN)
HU JIE (CN)
LIU ZHUGUO (CN)
HUANG YUANYUAN (CN)
DONG MINGXIN (CN)
YU ZHENG (CN)
HU JIE (CN)
LIU ZHUGUO (CN)
Application Number:
PCT/CN2008/001881
Publication Date:
May 20, 2010
Filing Date:
November 17, 2008
Export Citation:
Assignee:
BEIJING INST OF BIOTECHNOLOGY (CN)
DAI QIUYUN (CN)
HUANG YUANYUAN (CN)
DONG MINGXIN (CN)
YU ZHENG (CN)
HU JIE (CN)
LIU ZHUGUO (CN)
DAI QIUYUN (CN)
HUANG YUANYUAN (CN)
DONG MINGXIN (CN)
YU ZHENG (CN)
HU JIE (CN)
LIU ZHUGUO (CN)
International Classes:
C07K14/815; A61K38/55; A61K38/58; A61P7/02; C07K14/81; C12N15/15
Domestic Patent References:
| WO1990003391A1 | 1990-04-05 |
Foreign References:
| US5516656A | 1996-05-14 | |||
| CN101372512A | 2009-02-25 |
Other References:
PAUL BOURDON ET AL.: "Structure-function relationships ofhirulog peptide interactions with hrombin.", FEBS LETTERS., vol. 294, no. 3, December 1991 (1991-12-01), pages 164
VINCENZO DE FILIPPIS ET AL.: "Incorporation ofnoncoded amino acids into the N-terminal domain 1-47 of hirudin yields a highly potent and selective thrombin inhibitor.", PROTEIN SCIENCE., vol. 8, 1990, pages 2213 - 2217
VINCENZO DE FILIPPIS ET AL.: "Probing the hirudin-thrombin interaction by incorporation of noncoded amino acids and molecular dynamics simulation.", BIOCHEMISTRY, vol. 41, no. 46, 2002, pages 13556 - 13569
VINCENZO DE FILIPPIS ET AL.: "Incorporation ofnoncoded amino acids into the N-terminal domain 1-47 of hirudin yields a highly potent and selective thrombin inhibitor.", PROTEIN SCIENCE., vol. 8, 1990, pages 2213 - 2217
VINCENZO DE FILIPPIS ET AL.: "Probing the hirudin-thrombin interaction by incorporation of noncoded amino acids and molecular dynamics simulation.", BIOCHEMISTRY, vol. 41, no. 46, 2002, pages 13556 - 13569
Attorney, Agent or Firm:
JEEKAI & PARTNERS (Jinyu TowerA129 West Xuan Wu Men Street, Xicheng District, Beijing 1, CN)
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