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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
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pubmed:dateCreated |
1994-9-27
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pubmed:abstractText |
The sea anemone polypeptide anthopleurin-A (AP-A) at nanomolar concentrations enhances myocardial contractility without affecting automaticity. It has a therapeutic index higher than that of the digitalis glycosides, and may serve as a molecular model for designing a new class of inotropic drugs acting on the myocardial Na channel at site 3. AP-A is a 49 residue peptide crosslinked by three disulfide bonds; its tertiary structure has been determined by NMR. Here we report the solid-phase synthesis of this polypeptide. Synthetic AP-A displayed CD and NMR spectra identical with those of the natural toxin; it possessed 94 +/- 15% of the inotropic activity of natural AP-A. Therefore, it is feasible to prepare various type 1 sea anemone toxin analogs by solid-phase chemical synthesis in order to identify side chains important for peptide folding and interaction with sodium channels.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0367-8377
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
43
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
463-70
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8070970-Amino Acid Sequence,
pubmed-meshheading:8070970-Animals,
pubmed-meshheading:8070970-Atrial Function,
pubmed-meshheading:8070970-Cardiotonic Agents,
pubmed-meshheading:8070970-Circular Dichroism,
pubmed-meshheading:8070970-Electrophoresis,
pubmed-meshheading:8070970-Heart Atria,
pubmed-meshheading:8070970-Male,
pubmed-meshheading:8070970-Molecular Sequence Data,
pubmed-meshheading:8070970-Myocardial Contraction,
pubmed-meshheading:8070970-Peptides,
pubmed-meshheading:8070970-Rats,
pubmed-meshheading:8070970-Rats, Sprague-Dawley,
pubmed-meshheading:8070970-Sea Anemones,
pubmed-meshheading:8070970-Spectrometry, Mass, Fast Atom Bombardment
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pubmed:year |
1994
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pubmed:articleTitle |
Synthesis of the cardiac inotropic polypeptide anthopleurin-A.
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pubmed:affiliation |
Bachem Bioscience Inc., Department of Peptide Chemistry, Philadelphia, Pennsylvania.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, Non-U.S. Gov't
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