| In vitro inhibition of human renin by statine-containing tripeptide renin inhibitor (ES-1005). | |
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MedLine Citation:
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PMID: 2485069 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Dipeptide and tripeptide derivatives containing a statine residue were synthesized as human renin inhibitors. ES-305, bis[(1-naphthyl)methyl]acetyl-histidyl-statine-2(S)-methylbutylami de, was found to be a highly potent human renin inhibitor that is species-specific and enzyme-specific. The replacement of the methylbutylamide of ES-305 with the leucyl-lysinol (ES-1005) showed similar high potency against human renin (Ki value of 2.4 x 10(-9) M) and monkey renin (Ki value of 7.9 x 10(-9) M) as ES-305. ES-1005 competitively inhibited human renin. The compound was about one order of magnitude less potent against pig, dog, and rabbit renins. It had moderate inhibitory potencies against cathepsin D and pepsin (IC50 of cathepsin D and pepsin of 1.6 x 10(-5) and 8.0 x 10(-6) M, respectively). ES-1005, a newly synthesized tripeptide derivative containing statine, is a highly potent inhibitor of not only primate renin but also a wide variety of nonprimate renins. |
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Authors:
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T Kokubu; K Hiwada; E Murakami; S Muneta; Y Morisawa; Y Yabe; H Koike; Y Iijima |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Journal of cardiovascular pharmacology Volume: 10 Suppl 7 ISSN: 0160-2446 ISO Abbreviation: J. Cardiovasc. Pharmacol. Publication Date: 1987 |
Date Detail:
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Created Date: 1991-10-01 Completed Date: 1991-10-01 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 7902492 Medline TA: J Cardiovasc Pharmacol Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: S88-90 Citation Subset: IM |
Affiliation:
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2nd Department of Internal Medicine, Ehime University School of Medicine, Japan. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Dogs Goats Haplorhini Humans Oligopeptides / pharmacology* Protease Inhibitors Rabbits Rats Renin / antagonists & inhibitors* Swine |
| Chemical | |
Reg. No./Substance:
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0/Oligopeptides; 0/Protease Inhibitors; 115404-79-0/ES 1005; EC 3.4.23.15/Renin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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