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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1991-2-28
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pubmed:abstractText |
The synthetic antiprotease, FUT-175 (6-amidino-2-naphthyl-4-guanidinobenzoate), was found to be an extraordinarily potent and rapid inhibitor of human Q31 cytotoxic T-lymphocyte granzyme A. The granzyme A was inhibited in a time-dependent manner with kobs/i = 430,000 +/- 80,000 M-1 s-1. Four other FUT-175 analogs were also found to be potent, rapid Q31 granzyme A inhibitors. All five compounds inhibited Q31 cytotoxic T-lymphocyte-mediated cytolysis of human JY lymphoma cells, but at concentrations far in excess of those needed for granzyme A inhibition. The data presented suggest that postmarketing surveillance of FUT-175 should include a review of possible immunosuppressive side-effects, such as increased susceptibility to viral infections and to neoplastic transformations.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/GZMA protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Granzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Guanidines,
http://linkedlifedata.com/resource/pubmed/chemical/Serine Endopeptidases,
http://linkedlifedata.com/resource/pubmed/chemical/Serine Proteinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/nafamostat
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0003-9861
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
284
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
215-8
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1989498-Cytotoxicity, Immunologic,
pubmed-meshheading:1989498-Granzymes,
pubmed-meshheading:1989498-Guanidines,
pubmed-meshheading:1989498-Humans,
pubmed-meshheading:1989498-Immunity, Cellular,
pubmed-meshheading:1989498-Kinetics,
pubmed-meshheading:1989498-Serine Endopeptidases,
pubmed-meshheading:1989498-Serine Proteinase Inhibitors,
pubmed-meshheading:1989498-Structure-Activity Relationship,
pubmed-meshheading:1989498-T-Lymphocytes, Cytotoxic
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pubmed:year |
1991
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pubmed:articleTitle |
The enzymatic activity of human cytotoxic T-lymphocyte granzyme A and cytolysis mediated by cytotoxic T-lymphocytes are potently inhibited by a synthetic antiprotease, FUT-175.
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pubmed:affiliation |
Department of Enzymology, Merck Sharp and Dohme Research Laboratories, Rahway, New Jersey 07065.
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pubmed:publicationType |
Journal Article,
In Vitro
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