CX-397, A NOVEL RECOMBINANT HIRUDIN ANALOG HAVING A HYBRID SEQUENCE OF HIRUDIN VARIANT-1 AND VARIANT-3

被引：25

作者：

KOMATSU, Y ^{[1
]}

MISAWA, S ^{[1
]}

SUKESADA, A ^{[1
]}

OHBA, Y ^{[1
]}

HAYASHI, H ^{[1
]}

机构：

[1] NIKKO KYODO CO LTD,PHARMACEUT & BIOTECHNOL LAB,3-17-35 NIIZO MINAMI,TODA,SAITAMA 335,JAPAN

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1993年 / 196卷 / 02期

关键词：

D O I：

10.1006/bbrc.1993.2316

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

To elucidate the differential roles of N- and C-terminal halves of hirudins in thrombin inhibition, we produced novel recombinant hirudin analogs, CX-397 and CX-397R, having a hybrid amino acid sequence of hirudin variants-1 (HV-1) and -3 (HV-3). CX-397 is composed of the N-terminal half of HV-1 (HV-11-36) combined with the C-terminal half of HV-3 (HV-337-66). CX-397R is the opposite combination. Their anti-thrombin activity was determined by a fluorogenic enzyme assay and compared with that of recombinant HV-1 (rHV-1) and rHV-3. The order of the magnitude of dissociation constants (K(i)) of these four hirudin analogs in thrombin inhibition was as follows: CX-397R (0.294 pM) > rHV-1 (0.148 pM) > rHV-3 (0.0593 pM) > CX-397 (0.0433 pM), indicating that CS-397 is the strongest inhibitors among them. © 1993 Academic Press, Inc.

引用

页码：773 / 779

页数：7

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