Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4 Pt 1
pubmed:dateCreated
1991-11-18
pubmed:abstractText
The purpose of the present study was to investigate the relative roles of protein kinase C (PKC) and myosin light chain kinase (MLCK) in phorbol ester-induced contraction of vascular smooth muscle through the use of PKC and calmodulin antagonists. Prior exposure to PKC antagonists staurosporine (0.03 microM) and H-7 (10 microM) had relatively little effect on contractions to phorbol 12-myristate 13-acetate (PMA), while contractions to norepinephrine and KCl were greatly inhibited. Prior exposure to the calmodulin antagonists calmidazolium (3 and 10 microM) and W-7 (10 microM) inhibited contractions to PMA in the presence and absence of extracellular Ca2+, while contractions to norepinephrine and KCl remained relatively unaffected. Calmidazolium and W-7 were relatively weak relaxants when applied during the PMA contraction, and the magnitudes of relaxation were similar to those observed in norepinephrine- and KCl-contracted tissues. Calmidazolium partially inhibited the PMA-induced translocation of PKC. These results suggest that 1) the calmodulin antagonists inhibit the development of PMA-induced contraction, at least in part, through inhibition of PKC translocation; 2) the mechanisms of phorbol ester- and agonist-induced translocation of PKC are distinct; 3) the potencies and inhibitory mechanisms of these agents depend on whether the agents are added before or during the contraction; and 4) the selectivity of these agents, as evaluated in enzyme preparations, may not be consistent with their cellular actions.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Calcium, http://linkedlifedata.com/resource/pubmed/chemical/Calmodulin, http://linkedlifedata.com/resource/pubmed/chemical/Imidazoles, http://linkedlifedata.com/resource/pubmed/chemical/Isotonic Solutions, http://linkedlifedata.com/resource/pubmed/chemical/Krebs-Ringer solution, http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine, http://linkedlifedata.com/resource/pubmed/chemical/Potassium Chloride, http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase C, http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides, http://linkedlifedata.com/resource/pubmed/chemical/Tetradecanoylphorbol Acetate, http://linkedlifedata.com/resource/pubmed/chemical/W 7, http://linkedlifedata.com/resource/pubmed/chemical/calmidazolium
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
0002-9513
pubmed:author
pubmed:issnType
Print
pubmed:volume
261
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
C675-84
pubmed:dateRevised
2007-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Inhibition of phorbol ester-induced contraction by calmodulin antagonists in rat aorta.
pubmed:affiliation
Department of Pharmacology and Cell Biophysics, University of Cincinnati College of Medicine, Ohio 45267-0575.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S., Research Support, U.S. Gov't, Non-P.H.S., Research Support, Non-U.S. Gov't