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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
1999-12-9
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pubmed:abstractText |
Synthesis and anti-uPA activity of a series of Nalpha-triisopropyl-phenylsulfonyl-protected 3-amidinophenylalanine amides are described. We have explored SAR around the C-terminal amide part for inhibition of uPA, plasmin and trypsin. Modification of the amide part has been found to affect potency but not selectivity. With a Ki of 0.41 microM 2r-L is one of the most potent uPA inhibitors described so far. The X-ray crystal structure of 2r-L was solved in complex with trypsin, superimposed with uPA and the results suggest an unique binding mode of this inhibitor type.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
9
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3147-52
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:10560742-Benzamidines,
pubmed-meshheading:10560742-Enzyme Inhibitors,
pubmed-meshheading:10560742-Fibrinolysin,
pubmed-meshheading:10560742-Models, Molecular,
pubmed-meshheading:10560742-Molecular Conformation,
pubmed-meshheading:10560742-Molecular Structure,
pubmed-meshheading:10560742-Phenylalanine,
pubmed-meshheading:10560742-Structure-Activity Relationship,
pubmed-meshheading:10560742-Sulfonamides,
pubmed-meshheading:10560742-Trypsin Inhibitors,
pubmed-meshheading:10560742-Urokinase-Type Plasminogen Activator
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pubmed:year |
1999
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pubmed:articleTitle |
3-Amidinophenylalanine-based inhibitors of urokinase.
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pubmed:affiliation |
Zentrum f. Vaskuläre Biologie u. Medizin, Universität Jena, Erfurt, Germany. stuerze@zmkh.ef.uni-jena.de
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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