Literature DB >> 1310695

"Mirror image" antagonists of thrombin-induced platelet activation based on thrombin receptor structure.

D T Hung1, T K Vu, V I Wheaton, I F Charo, N A Nelken, N Esmon, C T Esmon, S R Coughlin.   

Abstract

Platelet activation by thrombin plays a critical role in hemostasis and thrombosis. Based on structure-activity studies of a cloned platelet thrombin receptor, we designed two "mirror image" antagonists of thrombin and thrombin receptor function. First, "uncleavable" peptides mimicking the receptor domain postulated to interact with thrombin were found to be potent thrombin inhibitors. Second, proteolytically inactive mutant thrombins designed to bind but not cleave the thrombin receptor were found to be specific antagonists of receptor activation by thrombin. The effectiveness of these designed antagonists in blocking thrombin-induced platelet activation suggests a model for thrombin-receptor interaction and possible strategies for the development of novel antithrombotic agents.

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Year:  1992        PMID： 1310695      PMCID： PMC442871          DOI： 10.1172/JCI115604

Source DB:  PubMed          Journal:  J Clin Invest        ISSN： 0021-9738            Impact factor:   14.808


  26 in total

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Authors:  T K Vu; D T Hung; V I Wheaton; S R Coughlin
Journal:  Cell       Date:  1991-03-22       Impact factor: 41.582

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Journal:  J Clin Invest       Date:  1977-10       Impact factor: 14.808

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Journal:  J Biol Chem       Date:  1974-04-25       Impact factor: 5.157

6.  Geometry of binding of the benzamidine- and arginine-based inhibitors N alpha-(2-naphthyl-sulphonyl-glycyl)-DL-p-amidinophenylalanyl-pipe ridine (NAPAP) and (2R,4R)-4-methyl-1-[N alpha-(3-methyl-1,2,3,4-tetrahydro-8- quinolinesulphonyl)-L-arginyl]-2-piperidine carboxylic acid (MQPA) to human alpha-thrombin. X-ray crystallographic determination of the NAPAP-trypsin complex and modeling of NAPAP-thrombin and MQPA-thrombin.

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Journal:  Eur J Biochem       Date:  1990-10-05

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Journal:  Thromb Res       Date:  1979       Impact factor: 3.944

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Journal:  J Biol Chem       Date:  1977-06-10       Impact factor: 5.157

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Journal:  J Biol Chem       Date:  1987-03-05       Impact factor: 5.157

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Authors:  R Laura; D J Robison; D H Bing
Journal:  Biochemistry       Date:  1980-10-14       Impact factor: 3.162
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  12 in total

Review 1.  How the protease thrombin talks to cells.

Authors:  S R Coughlin
Journal:  Proc Natl Acad Sci U S A       Date:  1999-09-28       Impact factor: 11.205

Review 2.  Characterization of a functional thrombin receptor. Issues and opportunities.

Authors:  S R Coughlin; T K Vu; D T Hung; V I Wheaton
Journal:  J Clin Invest       Date:  1992-02       Impact factor: 14.808

3.  Signalling pathways induced by protease-activated receptors and integrins in T cells.

Authors:  Rachel Bar-Shavit; Miriam Maoz; Yin Yongjun; Maya Groysman; Idit Dekel; Shulamit Katzav
Journal:  Immunology       Date:  2002-01       Impact factor: 7.397

Review 4.  Protease-activated receptors start a family.

Authors:  S R Coughlin
Journal:  Proc Natl Acad Sci U S A       Date:  1994-09-27       Impact factor: 11.205

5.  An essential role for SNX1 in lysosomal sorting of protease-activated receptor-1: evidence for retromer-, Hrs-, and Tsg101-independent functions of sorting nexins.

Authors:  Anuradha Gullapalli; Breann L Wolfe; Courtney T Griffin; Terry Magnuson; JoAnn Trejo
Journal:  Mol Biol Cell       Date:  2006-01-11       Impact factor: 4.138

6.  Cathepsin G and thrombin: evidence for two different platelet receptors.

Authors:  M A Selak
Journal:  Biochem J       Date:  1994-01-15       Impact factor: 3.857

Review 7.  Novel antithrombotic drugs in development.

Authors:  M Verstraete; P Zoldhelyi
Journal:  Drugs       Date:  1995-06       Impact factor: 9.546

8.  Thrombin receptor expression in normal and atherosclerotic human arteries.

Authors:  N A Nelken; S J Soifer; J O'Keefe; T K Vu; I F Charo; S R Coughlin
Journal:  J Clin Invest       Date:  1992-10       Impact factor: 14.808

9.  Different pathways for control of Na+/H+ exchange via activation of the thrombin receptor.

Authors:  R Nieuwland; G van Willigen; J W Akkerman
Journal:  Biochem J       Date:  1994-01-01       Impact factor: 3.857

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Journal:  Biochem J       Date:  1995-01-15       Impact factor: 3.857
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