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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1990-9-20
pubmed:abstractText
The binding and internalization of 125I-endothelin (125I-ET-1) was studied in cultured human vascular smooth muscle cells (hVSMC). Discrimination between surface-bound and internalized radiolabeled ligand was achieved using either acetic acid or trypsin treatment of cell layers, with the two procedures yielding comparable results. Total cellular 125I-ET-1 binding hVSMC at 37 degrees was rapid and reached near equilibrium within 30 min. Such binding could be resolved into surface-bound (acid/trypsin-sensitive) and internalized (acid/trypsin-resistant) components. The accumulation of internalized 125I-ET-1 was temperature dependent and occurred at 37 degrees (t1/2 approximately 15 min) but not at 4 degrees. Internalization of 125I-ET-1 by hVSMC was reversibly inhibited by the transglutaminase inhibitor dansylcadaverine (half-maximal inhibitory concentration, approximately 400 microM). Cytosolic acidification of hVSMC (from pH approximately 6.8 to approximately 6.3) by incubation with potassium acetate in a choline buffer also inhibited 125I-ET-1 internalization. Our observation indicate that smooth muscle cells internalize ET-1 via the clathrin-mediated endocytotic pathway. Dansylcadaverine and other inhibitors of transglutaminase inhibited ET-1-stimulated inositol phospholipid hydrolysis in hVSMC and decreased ET-1-induced vasoconstriction in isolated endothelium-denuded blood vessels. Internalization of ET-1 may, therefore, be relevant to the characteristically protracted physiological effects of this peptide on the vasculature.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0026-895X
pubmed:author
pubmed:issnType
Print
pubmed:volume
38
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
244-52
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Internalization of endothelin by cultured human vascular smooth muscle cells: characterization and physiological significance.
pubmed:affiliation
Department of Research, University Hospital, Basel, Switzerland.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't