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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1991-3-15
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pubmed:abstractText |
1. We describe the results of a structure-activity study in which the C-terminal hexapeptide of the endothelins, endothelin (16-21), is compared with shorter fragments; hexapeptides bearing amino-acid substitutions and the corresponding C-terminal fragments of sarafotoxins. The guinea-pig bronchus was used in this study since it is the most sensitive preparation for endothelin (16-21) thus far developed. 2. The biological results obtained with endothelin (16-21) and analogues demonstrate that the contractile activity of the C-terminal hexapeptide of endothelin on the guinea-pig bronchus depends on quite close structural requirements, strongly suggestive of a receptor interaction. The following features appear to be essential for the biological activity: (a) the C-terminal free carboxylic function; (b) the L-configuration of Trp-21; (c) the beta-carboxylic function of Asp-18; (d) the presence of Leu-17 and (e) the imidazole moiety of His-16. 3. The hexapeptide corresponding to the C-terminal portion of sarafotoxin, sarafotoxin (16-21), was devoid of biological activity. This behaviour might be related to the proposed existence of more than one receptor for the endothelin/sarafotoxin family in the guinea-pig bronchus.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2178945,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2451132,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2473297,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2473306,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2473328,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2473337,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2476324,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2536275,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2547655,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2549664,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2553427,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2646136,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2646137,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2649896,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2663109,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2663526,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2673240,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2673799,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2684315,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2693125,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2845579,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-2907490,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3045827,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3056409,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3059352,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3065091,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3068063,
http://linkedlifedata.com/resource/pubmed/commentcorrection/2282462-3072211
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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 |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
101
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
232-4
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:2282462-Amino Acid Sequence,
pubmed-meshheading:2282462-Animals,
pubmed-meshheading:2282462-Bronchi,
pubmed-meshheading:2282462-Endothelins,
pubmed-meshheading:2282462-Guinea Pigs,
pubmed-meshheading:2282462-Male,
pubmed-meshheading:2282462-Molecular Sequence Data,
pubmed-meshheading:2282462-Muscle, Smooth,
pubmed-meshheading:2282462-Muscle Contraction,
pubmed-meshheading:2282462-Peptide Fragments,
pubmed-meshheading:2282462-Peptides,
pubmed-meshheading:2282462-Structure-Activity Relationship,
pubmed-meshheading:2282462-Vasoconstrictor Agents,
pubmed-meshheading:2282462-Viper Venoms
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pubmed:year |
1990
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pubmed:articleTitle |
Structure-activity studies on endothelin (16-21), the C-terminal hexapeptide of the endothelins, in the guinea-pig bronchus.
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pubmed:affiliation |
Chemistry Department, A. Menarini Pharmaceuticals, Firenze, Italy.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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