Mapping the interaction of bradykinin 1-5 with the exodomain of human protease activated receptor 4

被引:13
作者
Nieman, MT
Pagan-Ramo, E
Warnock, M
Krijanovski, Y
Hasan, AAK
Schmaier, AH [1 ]
机构
[1] Univ Michigan, Dept Internal Med, Ann Arbor, MI 48109 USA
[2] Thromgen Inc, Ann Arbor, MI 48104 USA
来源
FEBS LETTERS | 2005年 / 579卷 / 01期
关键词
thrombin; PAR4; bradykinin; 1-5; RPPGF;
D O I
10.1016/j.febslet.2004.11.041
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
The angiotensin converting enzyme breakdown product of bradykinin, bradykinin 1-5 (RPPGF), inhibits thrombin-induced human or mouse platelet aggregation. RPPGF binds to the exodomain of human protease-activated receptor 1 (PAR1). Studies determined if RPPGF also binds to the exodomain of human PAR4. RPPGF binds to a peptide of the thrombin cleavage site on PAR4. Recombinant wild-type and mutated exodomain of human PAR4 was prepared. The N-terminal arginine on RPPGF binds to the P2 position or proline 46 on PAR4 to block thrombin cleavage. These data indicate that RPPGF influences thrombin activity by binding to the thrombin cleavage site on both PAR4 and PAR1 (C) 2004 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.
引用
收藏
页码:25 / 29
页数:5
相关论文
共 22 条
[1]   Thrombin and platelet activation [J].
Brass, LF .
CHEST, 2003, 124 (03) :18S-25S
[2]   Establishing the inhibitory effects of bradykinin on thrombin [J].
Cleary, DB ;
Ehringer, WD ;
Maurer, MC .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 2003, 410 (01) :96-106
[3]   Protease-activated receptor 4-like peptides bind to thrombin through an optimized interaction with the enzyme active site surface [J].
Cleary, DB ;
Trumbo, TA ;
Maurer, MC .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 2002, 403 (02) :179-188
[4]   How the protease thrombin talks to cells [J].
Coughlin, SR .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1999, 96 (20) :11023-11027
[5]   Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets [J].
Covic, L ;
Gresser, AL ;
Kuliopulos, A .
BIOCHEMISTRY, 2000, 39 (18) :5458-5467
[6]   Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation [J].
Covic, L ;
Misra, M ;
Badar, J ;
Singh, C ;
Kuliopulos, A .
NATURE MEDICINE, 2002, 8 (10) :1161-1165
[7]   Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates [J].
Derian, CK ;
Damiano, BP ;
Addo, MF ;
Darrow, AL ;
D'Andrea, MR ;
Nedelman, M ;
Zhang, HC ;
Maryanoff, BE ;
Andrade-Gordon, P .
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2003, 304 (02) :855-861
[8]  
HASAN AAK, 1994, J BIOL CHEM, V269, P31822
[9]   Mechanisms of Arg-Pro-Pro-Gly-Phe inhibition of thrombin [J].
Hasan, AAK ;
Warnock, M ;
Nieman, M ;
Srikanth, S ;
Mahdi, F ;
Krishnan, R ;
Tulinsky, A ;
Schmaier, AH .
AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY, 2003, 285 (01) :H183-H193
[10]   Bradykinin and its metabolite, Arg-Pro-Pro-Gly. Phe, are selective inhibitors of alpha-thrombin-induced platelet activation [J].
Hasan, AAK ;
Amenta, S ;
Schmaier, AH .
CIRCULATION, 1996, 94 (03) :517-528