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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2009-3-16
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pubmed:abstractText |
A novel series of matriptase inhibitors based on previously identified tribasic 3-amidinophenylalanine derivatives was prepared. The C-terminal basic group was replaced by neutral residues to reduce the hydrophilicity of the inhibitors. The most potent compound 22 inhibits matriptase with a K(i) value of 0.43 nM, but lacks selectivity towards factor Xa. By combination with neutral N-terminal sulfonyl residues several potent thrombin inhibitors were identified, which had reduced matriptase affinity.
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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 |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1960-5
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pubmed:meshHeading |
pubmed-meshheading:19250826-Administration, Oral,
pubmed-meshheading:19250826-Amidines,
pubmed-meshheading:19250826-Animals,
pubmed-meshheading:19250826-Factor Xa,
pubmed-meshheading:19250826-Phenylalanine,
pubmed-meshheading:19250826-Rats,
pubmed-meshheading:19250826-Serine Endopeptidases,
pubmed-meshheading:19250826-Serine Proteinase Inhibitors,
pubmed-meshheading:19250826-Sulfonamides,
pubmed-meshheading:19250826-Thrombin
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pubmed:year |
2009
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pubmed:articleTitle |
Incorporation of neutral C-terminal residues in 3-amidinophenylalanine-derived matriptase inhibitors.
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pubmed:affiliation |
The Medicines Company (Leipzig) GmbH, Deutscher Platz 5d, D-04103 Leipzig, Germany.
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pubmed:publicationType |
Journal Article
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