| pubmed-article:1871142 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C0079281 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C2709248 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C0042396 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C0205369 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:1871142 | lifeskim:mentions | umls-concept:C1707689 | lld:lifeskim |
| pubmed-article:1871142 | pubmed:issue | 16 | lld:pubmed |
| pubmed-article:1871142 | pubmed:dateCreated | 1991-9-18 | lld:pubmed |
| pubmed-article:1871142 | pubmed:abstractText | The 21-amino acid vasoconstrictor peptide endothelin (Et) contains two disulfide bonds. We investigated the importance of the outer disulfide bond in Et-1 by replacing it with an amide linkage. Bioactivity was assessed in an isolated guinea pig lung preparation (perfused at constant flow with Ringer's solution/0.5% albumin) in which pulmonary artery pressure was monitored. Et-1 produced concentration-dependent pulmonary vasoconstriction at concentrations of 1 x 10(-10) M and higher. [Dpr1, Asp15]Et-1 (where Dpr is diaminopropionic acid), in which the outer disulfide was replaced by an amide bond and the inner disulfide was left intact, showed no agonist activity at 1 x 10(-6) M but 1 x 10(-7) M [Dpr1, Asp15]Et-1 inhibited Et-1-induced pulmonary vasoconstriction: effects of 1 x 10(-10) M 2 x 10(-10) M, and 1 x 10(-9) M Et-1 were inhibited by 98%, 75%, and 65%, respectively. Furthermore, this analog did not alter pulmonary vasoconstriction induced by thrombin, norepinephrine, or, most significantly, Et-3. A monocyclic Et-1 analog with the same sequence but in which the amide bond was not formed showed weak pulmonary vasoconstrictor activity (300-500 times less potent than Et-1) but had no antagonist activity. In addition, both the monocyclic control peptide and [Dpr1, Asp15]Et-1 competed effectively with 125I-labeled Et-1 for binding to cultured rat pulmonary artery smooth muscle cells. Thus, an Et-1 structural analog produced by replacement of the outer disulfide bond with an amide linkage displayed potent and specific Et-1 antagonism. | lld:pubmed |
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| pubmed-article:1871142 | pubmed:language | eng | lld:pubmed |
| pubmed-article:1871142 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:1871142 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:1871142 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:1871142 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:1871142 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:1871142 | pubmed:issn | 0027-8424 | lld:pubmed |
| pubmed-article:1871142 | pubmed:author | pubmed-author:MalikA BAB | lld:pubmed |
| pubmed-article:1871142 | pubmed:author | pubmed-author:EverittJJ | lld:pubmed |
| pubmed-article:1871142 | pubmed:author | pubmed-author:AndersenT TTT | lld:pubmed |
| pubmed-article:1871142 | pubmed:author | pubmed-author:SpinellaM JMJ | lld:pubmed |
| pubmed-article:1871142 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:1871142 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:1871142 | pubmed:volume | 88 | lld:pubmed |
| pubmed-article:1871142 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:1871142 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:1871142 | pubmed:pagination | 7443-6 | lld:pubmed |
| pubmed-article:1871142 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:1871142 | pubmed:year | 1991 | lld:pubmed |
| pubmed-article:1871142 | pubmed:articleTitle | Design and synthesis of a specific endothelin 1 antagonist: effects on pulmonary vasoconstriction. | lld:pubmed |
| pubmed-article:1871142 | pubmed:affiliation | Department of Biochemistry and Molecular Biology, Albany Medical College of Union University, NY 12208. | lld:pubmed |
| pubmed-article:1871142 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:1871142 | pubmed:publicationType | In Vitro | lld:pubmed |
| pubmed-article:1871142 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:1871142 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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