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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
1987-10-9
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pubmed:abstractText |
The pentapeptide BOC-Phe-Phe-difluorostatone-Leu-Phe-NH2 has been prepared and found to be a potent inhibitor of human renin. This compound contains a difluoromethylene ketone group that exists predominantly in the hydrated form in water. The difluorostatone-containing peptide is 7-fold and 22-fold more potent than the analogous statine- and statone-containing peptides, respectively. Structure/activity analysis of the most potent inhibitor was carried out by replacing some of the peptide bonds with trans-alkenes. In all cases, a dramatic loss in binding to renin was observed. A number of statine-containing inhibitors of renin have been reported and this work suggests that the replacement of statine with difluorostatone will yield more potent compounds.
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pubmed:grant |
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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 |
Sep
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1617-22
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
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pubmed:year |
1987
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pubmed:articleTitle |
Fluoro ketone containing peptides as inhibitors of human renin.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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