Enhanced endothelin ETB receptor down-regulation in human tumor cells
Identifieur interne : 002463 ( Main/Exploration ); précédent : 002462; suivant : 002464Enhanced endothelin ETB receptor down-regulation in human tumor cells
Auteurs : Jan Drimal [Slovaquie] ; Jan Drimal Jr ; Daniel DrimalSource :
- European Journal of Pharmacology [ 0014-2999 ] ; 2000.
English descriptors
- Teeft :
- Agonist, Analogue, Binding sites, Bmax, Chloroquine, Drimal, Endothelin, Endothelin receptor agonists, Endothelin receptors, European journal, Fibroblast, Hela, Hela cells, Human cells, Human fibroblasts, Hxthymidine, Hxthymidine incorporation, Ixtyr, Ligand, Neoplastic, Nmolrl, Peptide, Pharmacology, Present study, Receptor, Relative density, Specific activity, Specific binding, Tumor cells, Tumorigenic, Tumorigenic cells.
Abstract
Abstract: The characteristics of specific binding of human [125I]Tyr13-endothelin-(1–21), [125I]-Tyr13-Suc-[Glu9,Ala11,15]-endothelin-(8–21), ([125I]IRL-1620) and endothelin ETA receptor antagonist [125I]Tyr3-(N-[(hexahydro-1H-azepin-1-yl)carbonyl]-l-Leu]-1Me)-d-Trp ([125I]PD151242) (number of sites and their affinity) and proliferation responses to exogenous endothelin receptor agonists (endothelin-1 and the endothelin ETB receptor-selective, truncated N-acetyl-[Ala11,15]-endothelin-(6–21) analogue BQ3020) were determined in cultured human fibroblasts and in tumorigenic HeLa cells. The cells were pre-incubated with equimolar concentrations of human endothelin-1 or its truncated analogue BQ3020. After pre-incubation (2 h), both peptides induced down-regulation of surface-membrane endothelin-1 receptors. This process was specific for endothelin ETB receptors and was much more intensive in tumorigenic cells. BQ3020, acting mostly through its C-terminus, induced nearly maximal endothelin ETB receptor down-regulation in HeLa cells. Staurosporine, a wide spectrum protein kinase inhibitor, significantly reduced, and N-[N-[N-[2,6-dimethyl-1piperidinyl)carbonyl]-4-Me-l-Leu]-1-(methoxycarbonyl)-d-tryptophanyl]-d-norleucine (BQ788), an endothelin ETB receptor antagonist, attenuated the down-regulation of endothelin receptors induced by endothelin receptor agonists. The down-regulation of endothelin ETB receptors was prevented by pre-incubation of the cells with the lysosomal enzyme blocker chloroquine. The endothelin-1-induced cell proliferation was attenuated by pre-incubation of the cells with the non-selective endothelin receptor antagonist Ac-d-10,11-dihydro-5H-dibenzo[a,d] cycloheptene-glycine-3,3-d-diphenyl-Ala-Leu-Asp-Ile-Ile-Trp (PD142893) and it was only partially reduced by the endothelin ETA receptor-selective endothelin antagonist PD151242.
Url:
DOI: 10.1016/S0014-2999(00)00198-9
Affiliations:
Links toward previous steps (curation, corpus...)
- to stream Istex, to step Corpus: 000F98
- to stream Istex, to step Curation: 000F98
- to stream Istex, to step Checkpoint: 001280
- to stream Main, to step Merge: 002491
- to stream Main, to step Curation: 002463
Le document en format XML
<record><TEI wicri:istexFullTextTei="biblStruct"><teiHeader><fileDesc><titleStmt><title>Enhanced endothelin ETB receptor down-regulation in human tumor cells</title><author><name sortKey="Drimal, Jan" sort="Drimal, Jan" uniqKey="Drimal J" first="Jan" last="Drimal">Jan Drimal</name></author><author><name sortKey="Drimal Jr, Jan" sort="Drimal Jr, Jan" uniqKey="Drimal Jr J" first="Jan" last="Drimal Jr">Jan Drimal Jr</name></author><author><name sortKey="Drimal, Daniel" sort="Drimal, Daniel" uniqKey="Drimal D" first="Daniel" last="Drimal">Daniel Drimal</name></author></titleStmt><publicationStmt><idno type="wicri:source">ISTEX</idno><idno type="RBID">ISTEX:4E0E76FB81F50348B32F1CCECBC4B4C513F83127</idno><date when="2000" year="2000">2000</date><idno type="doi">10.1016/S0014-2999(00)00198-9</idno><idno type="url">https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/fulltext.pdf</idno><idno type="wicri:Area/Istex/Corpus">000F98</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Corpus" wicri:corpus="ISTEX">000F98</idno><idno type="wicri:Area/Istex/Curation">000F98</idno><idno type="wicri:Area/Istex/Checkpoint">001280</idno><idno type="wicri:explorRef" wicri:stream="Istex" wicri:step="Checkpoint">001280</idno><idno type="wicri:doubleKey">0014-2999:2000:Drimal J:enhanced:endothelin:etb</idno><idno type="wicri:Area/Main/Merge">002491</idno><idno type="wicri:Area/Main/Curation">002463</idno><idno type="wicri:Area/Main/Exploration">002463</idno></publicationStmt><sourceDesc><biblStruct><analytic><title level="a">Enhanced endothelin ETB receptor down-regulation in human tumor cells</title><author><name sortKey="Drimal, Jan" sort="Drimal, Jan" uniqKey="Drimal J" first="Jan" last="Drimal">Jan Drimal</name><affiliation wicri:level="1"><country wicri:rule="url">Slovaquie</country></affiliation><affiliation></affiliation></author><author><name sortKey="Drimal Jr, Jan" sort="Drimal Jr, Jan" uniqKey="Drimal Jr J" first="Jan" last="Drimal Jr">Jan Drimal Jr</name><affiliation><wicri:noCountry code="subField">Republic</wicri:noCountry></affiliation></author><author><name sortKey="Drimal, Daniel" sort="Drimal, Daniel" uniqKey="Drimal D" first="Daniel" last="Drimal">Daniel Drimal</name><affiliation><wicri:noCountry code="subField">Republic</wicri:noCountry></affiliation></author></analytic><monogr></monogr><series><title level="j">European Journal of Pharmacology</title><title level="j" type="abbrev">EJP</title><idno type="ISSN">0014-2999</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="2000">2000</date><biblScope unit="volume">396</biblScope><biblScope unit="issue">1</biblScope><biblScope unit="page" from="19">19</biblScope><biblScope unit="page" to="22">22</biblScope></imprint><idno type="ISSN">0014-2999</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0014-2999</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Agonist</term><term>Analogue</term><term>Binding sites</term><term>Bmax</term><term>Chloroquine</term><term>Drimal</term><term>Endothelin</term><term>Endothelin receptor agonists</term><term>Endothelin receptors</term><term>European journal</term><term>Fibroblast</term><term>Hela</term><term>Hela cells</term><term>Human cells</term><term>Human fibroblasts</term><term>Hxthymidine</term><term>Hxthymidine incorporation</term><term>Ixtyr</term><term>Ligand</term><term>Neoplastic</term><term>Nmolrl</term><term>Peptide</term><term>Pharmacology</term><term>Present study</term><term>Receptor</term><term>Relative density</term><term>Specific activity</term><term>Specific binding</term><term>Tumor cells</term><term>Tumorigenic</term><term>Tumorigenic cells</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Abstract: The characteristics of specific binding of human [125I]Tyr13-endothelin-(1–21), [125I]-Tyr13-Suc-[Glu9,Ala11,15]-endothelin-(8–21), ([125I]IRL-1620) and endothelin ETA receptor antagonist [125I]Tyr3-(N-[(hexahydro-1H-azepin-1-yl)carbonyl]-l-Leu]-1Me)-d-Trp ([125I]PD151242) (number of sites and their affinity) and proliferation responses to exogenous endothelin receptor agonists (endothelin-1 and the endothelin ETB receptor-selective, truncated N-acetyl-[Ala11,15]-endothelin-(6–21) analogue BQ3020) were determined in cultured human fibroblasts and in tumorigenic HeLa cells. The cells were pre-incubated with equimolar concentrations of human endothelin-1 or its truncated analogue BQ3020. After pre-incubation (2 h), both peptides induced down-regulation of surface-membrane endothelin-1 receptors. This process was specific for endothelin ETB receptors and was much more intensive in tumorigenic cells. BQ3020, acting mostly through its C-terminus, induced nearly maximal endothelin ETB receptor down-regulation in HeLa cells. Staurosporine, a wide spectrum protein kinase inhibitor, significantly reduced, and N-[N-[N-[2,6-dimethyl-1piperidinyl)carbonyl]-4-Me-l-Leu]-1-(methoxycarbonyl)-d-tryptophanyl]-d-norleucine (BQ788), an endothelin ETB receptor antagonist, attenuated the down-regulation of endothelin receptors induced by endothelin receptor agonists. The down-regulation of endothelin ETB receptors was prevented by pre-incubation of the cells with the lysosomal enzyme blocker chloroquine. The endothelin-1-induced cell proliferation was attenuated by pre-incubation of the cells with the non-selective endothelin receptor antagonist Ac-d-10,11-dihydro-5H-dibenzo[a,d] cycloheptene-glycine-3,3-d-diphenyl-Ala-Leu-Asp-Ile-Ile-Trp (PD142893) and it was only partially reduced by the endothelin ETA receptor-selective endothelin antagonist PD151242.</div></front></TEI><affiliations><list><country><li>Slovaquie</li></country></list><tree><noCountry><name sortKey="Drimal Jr, Jan" sort="Drimal Jr, Jan" uniqKey="Drimal Jr J" first="Jan" last="Drimal Jr">Jan Drimal Jr</name><name sortKey="Drimal, Daniel" sort="Drimal, Daniel" uniqKey="Drimal D" first="Daniel" last="Drimal">Daniel Drimal</name></noCountry><country name="Slovaquie"><noRegion><name sortKey="Drimal, Jan" sort="Drimal, Jan" uniqKey="Drimal J" first="Jan" last="Drimal">Jan Drimal</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=$WICRI_ROOT/Sante/explor/ChloroquineV1/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 002463 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 002463 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= Sante
|area= ChloroquineV1
|flux= Main
|étape= Exploration
|type= RBID
|clé= ISTEX:4E0E76FB81F50348B32F1CCECBC4B4C513F83127
|texte= Enhanced endothelin ETB receptor down-regulation in human tumor cells
}}
| This area was generated with Dilib version V0.6.33. |  |