Enhanced endothelin ETB receptor down-regulation in human tumor cells
Identifieur interne : 000F98 ( Istex/Corpus ); précédent : 000F97; suivant : 000F99Enhanced endothelin ETB receptor down-regulation in human tumor cells
Auteurs : Jan Drimal ; 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
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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><istex><corpusName>elsevier</corpusName><keywords><teeft><json:string>endothelin</json:string><json:string>receptor</json:string><json:string>hela</json:string><json:string>fibroblast</json:string><json:string>hela cells</json:string><json:string>human fibroblasts</json:string><json:string>drimal</json:string><json:string>agonist</json:string><json:string>nmolrl</json:string><json:string>endothelin receptors</json:string><json:string>tumorigenic</json:string><json:string>pharmacology</json:string><json:string>hxthymidine</json:string><json:string>bmax</json:string><json:string>binding sites</json:string><json:string>specific binding</json:string><json:string>ixtyr</json:string><json:string>chloroquine</json:string><json:string>present study</json:string><json:string>european journal</json:string><json:string>neoplastic</json:string><json:string>specific activity</json:string><json:string>human cells</json:string><json:string>endothelin receptor agonists</json:string><json:string>tumorigenic cells</json:string><json:string>hxthymidine incorporation</json:string><json:string>relative density</json:string><json:string>tumor cells</json:string><json:string>ligand</json:string><json:string>analogue</json:string><json:string>peptide</json:string></teeft></keywords><author><json:item><name>Jan Drimal</name><affiliations><json:string>E-mail: exfadrim@savba.sk</json:string><json:string>Institute of Experimental Pharmacology, Cardiovascular Research Laboratory, Slovak Academy of Sciences, Dubravska cesta 9, 842 16 Bratislava, Slovak Republic</json:string></affiliations></json:item><json:item><name>Jan Drimal, Jr</name><affiliations><json:string>Department of Information Technologies, Slovak Gas Industry, Bratislava, Slovak Republic</json:string></affiliations></json:item><json:item><name>Daniel Drimal</name><affiliations><json:string>Faculty of Material Science and Technology, Slovak University of Technology, Bratislava, Slovak Republic</json:string></affiliations></json:item></author><subject><json:item><lang><json:string>eng</json:string></lang><value>Endothelin ETA receptor</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>Endothelin ETB receptor</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>Fibroblast</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>(Human)</value></json:item><json:item><lang><json:string>eng</json:string></lang><value>HeLa cell</value></json:item></subject><arkIstex>ark:/67375/6H6-DHK4H0C7-6</arkIstex><language><json:string>eng</json:string></language><originalGenre><json:string>Short communication</json:string></originalGenre><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.</abstract><qualityIndicators><score>6.559</score><pdfWordCount>2243</pdfWordCount><pdfCharCount>15169</pdfCharCount><pdfVersion>1.2</pdfVersion><pdfPageCount>4</pdfPageCount><pdfPageSize>595 x 758 pts</pdfPageSize><refBibsNative>true</refBibsNative><abstractWordCount>193</abstractWordCount><abstractCharCount>1874</abstractCharCount><keywordCount>5</keywordCount></qualityIndicators><title>Enhanced endothelin ETB receptor down-regulation in human tumor cells</title><pmid><json:string>10822048</json:string></pmid><pii><json:string>S0014-2999(00)00198-9</json:string></pii><genre><json:string>brief-communication</json:string></genre><host><title>European Journal of Pharmacology</title><language><json:string>unknown</json:string></language><publicationDate>2000</publicationDate><issn><json:string>0014-2999</json:string></issn><pii><json:string>S0014-2999(00)X0256-7</json:string></pii><volume>396</volume><issue>1</issue><pages><first>19</first><last>22</last></pages><genre><json:string>journal</json:string></genre></host><namedEntities><unitex><date><json:string>2000</json:string></date><geogName></geogName><orgName><json:string>Department of Information Technologies</json:string><json:string>Institute of Virology ŽSAS</json:string><json:string>Research Laboratory</json:string><json:string>Institute of Virology, Slovak Academy of Sciences</json:string><json:string>Ministry of Education of the Slovak Republic</json:string><json:string>Grants VEGA No</json:string></orgName><orgName_funder><json:string>Ministry of Education of the Slovak Republic</json:string><json:string>Grants VEGA No</json:string></orgName_funder><orgName_provider></orgName_provider><persName><json:string>Ždata</json:string><json:string>L. 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Drimal et al.</json:string><json:string>Drimal et al., 1999</json:string></ref_bibl><bibl></bibl></unitex></namedEntities><ark><json:string>ark:/67375/6H6-DHK4H0C7-6</json:string></ark><categories><wos><json:string>1 - science</json:string><json:string>2 - pharmacology & pharmacy</json:string></wos><scienceMetrix><json:string>1 - health sciences</json:string><json:string>2 - clinical medicine</json:string><json:string>3 - pharmacology & pharmacy</json:string></scienceMetrix><scopus><json:string>1 - Life Sciences</json:string><json:string>2 - Pharmacology, Toxicology and Pharmaceutics</json:string><json:string>3 - Pharmacology</json:string></scopus><inist><json:string>1 - sciences appliquees, technologies et medecines</json:string><json:string>2 - sciences biologiques et medicales</json:string><json:string>3 - sciences medicales</json:string><json:string>4 - tumeurs</json:string></inist></categories><publicationDate>2000</publicationDate><copyrightDate>2000</copyrightDate><doi><json:string>10.1016/S0014-2999(00)00198-9</json:string></doi><id>4E0E76FB81F50348B32F1CCECBC4B4C513F83127</id><score>1</score><fulltext><json:item><extension>pdf</extension><original>true</original><mimetype>application/pdf</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/fulltext.pdf</uri></json:item><json:item><extension>zip</extension><original>false</original><mimetype>application/zip</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/bundle.zip</uri></json:item><istex:fulltextTEI uri="https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/fulltext.tei"><teiHeader><fileDesc><titleStmt><title level="a">Enhanced endothelin ETB receptor down-regulation in human tumor cells</title></titleStmt><publicationStmt><authority>ISTEX</authority><publisher scheme="https://scientific-publisher.data.istex.fr">ELSEVIER</publisher><availability><licence><p>©2000 Elsevier Science B.V.</p></licence><p scheme="https://loaded-corpus.data.istex.fr/ark:/67375/XBH-HKKZVM7B-M">elsevier</p></availability><date>2000</date></publicationStmt><notesStmt><note type="brief-communication" scheme="https://content-type.data.istex.fr/ark:/67375/XTP-S9SX2MFS-0">brief-communication</note><note type="journal" scheme="https://publication-type.data.istex.fr/ark:/67375/JMC-0GLKJH51-B">journal</note><note type="content">Section title: Short communication</note><note type="content">Table 1: The intensity of down-regulation of endothelin receptors on cultured normal and tumorigenic human cells With the nonselective human endothelin-1 and with the endothelin ETB receptor-selective, truncated endothelin-1-(6–21) analogue, linear peptide BQ3020. Characteristics of binding of radioactive ligands [125I]endothelin-1 with preferential affinity for endothelin ETA receptors (ETA≫ETB) and truncated (endothelin-1-(8–21) ligand [125I]IRL-1620, with preferential affinity for endothelin ETB receptors (ETB≫ETA). Measured parameters: (D) Surface endothelin receptor density; (A) Affinity, expressed here as Kd; and (P) Proliferative response ([3H]thymidine incorporation) are expressed as percentages of control. Values are Means±S.E.M., (n=24).</note></notesStmt><sourceDesc><biblStruct type="inbook"><analytic><title level="a">Enhanced endothelin ETB receptor down-regulation in human tumor cells</title><author xml:id="author-0000"><persName><forename type="first">Jan</forename><surname>Drimal</surname></persName><email>exfadrim@savba.sk</email><note type="correspondence"><p>Corresponding author. Tel.: +42-07-59410660; fax: +42-07-54775928</p></note><affiliation>Institute of Experimental Pharmacology, Cardiovascular Research Laboratory, Slovak Academy of Sciences, Dubravska cesta 9, 842 16 Bratislava, Slovak Republic</affiliation></author><author xml:id="author-0001"><persName><forename type="first">Jan</forename><surname>Drimal, Jr</surname></persName><affiliation>Department of Information Technologies, Slovak Gas Industry, Bratislava, Slovak Republic</affiliation></author><author xml:id="author-0002"><persName><forename type="first">Daniel</forename><surname>Drimal</surname></persName><affiliation>Faculty of Material Science and Technology, Slovak University of Technology, Bratislava, Slovak Republic</affiliation></author><idno type="istex">4E0E76FB81F50348B32F1CCECBC4B4C513F83127</idno><idno type="ark">ark:/67375/6H6-DHK4H0C7-6</idno><idno type="DOI">10.1016/S0014-2999(00)00198-9</idno><idno type="PII">S0014-2999(00)00198-9</idno></analytic><monogr><title level="j">European Journal of Pharmacology</title><title level="j" type="abbrev">EJP</title><idno type="pISSN">0014-2999</idno><idno type="PII">S0014-2999(00)X0256-7</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="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></monogr></biblStruct></sourceDesc></fileDesc><profileDesc><creation><date>2000</date></creation><langUsage><language ident="en">en</language></langUsage><abstract xml:lang="en"><p>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.</p></abstract><textClass><keywords scheme="keyword"><list><head>Keywords</head><item><term>Endothelin ETA receptor</term></item><item><term>Endothelin ETB receptor</term></item><item><term>Fibroblast</term></item><item><term>(Human)</term></item><item><term>HeLa cell</term></item></list></keywords></textClass></profileDesc><revisionDesc><change when="2000-03-02">Modified</change><change when="2000">Published</change></revisionDesc></teiHeader></istex:fulltextTEI><json:item><extension>txt</extension><original>false</original><mimetype>text/plain</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/fulltext.txt</uri></json:item></fulltext><metadata><istex:metadataXml wicri:clean="Elsevier, elements deleted: ce:floats; body; tail"><istex:xmlDeclaration>version="1.0" encoding="utf-8"</istex:xmlDeclaration><istex:docType PUBLIC="-//ES//DTD journal article DTD version 4.5.2//EN//XML" URI="art452.dtd" name="istex:docType"></istex:docType><istex:document><converted-article version="4.5.2" docsubtype="sco"><item-info><jid>EJP</jid><aid>58751</aid><ce:pii>S0014-2999(00)00198-9</ce:pii><ce:doi>10.1016/S0014-2999(00)00198-9</ce:doi><ce:copyright type="full-transfer" year="2000">Elsevier Science B.V.</ce:copyright></item-info><head><ce:dochead><ce:textfn>Short communication</ce:textfn></ce:dochead><ce:title>Enhanced endothelin ET<ce:inf>B</ce:inf> receptor down-regulation in human tumor cells</ce:title><ce:author-group><ce:author><ce:given-name>Jan</ce:given-name><ce:surname>Drimal</ce:surname><ce:cross-ref refid="AFF1"><ce:sup>a</ce:sup></ce:cross-ref><ce:cross-ref refid="CORR1">*</ce:cross-ref><ce:e-address>exfadrim@savba.sk</ce:e-address></ce:author><ce:author><ce:given-name>Jan</ce:given-name><ce:surname>Drimal</ce:surname><ce:suffix>Jr</ce:suffix><ce:cross-ref refid="AFF2"><ce:sup>b</ce:sup></ce:cross-ref></ce:author><ce:author><ce:given-name>Daniel</ce:given-name><ce:surname>Drimal</ce:surname><ce:cross-ref refid="AFF3"><ce:sup>c</ce:sup></ce:cross-ref></ce:author><ce:affiliation id="AFF1"><ce:label>a</ce:label><ce:textfn>Institute of Experimental Pharmacology, Cardiovascular Research Laboratory, Slovak Academy of Sciences, Dubravska cesta 9, 842 16 Bratislava, Slovak Republic</ce:textfn></ce:affiliation><ce:affiliation id="AFF2"><ce:label>b</ce:label><ce:textfn>Department of Information Technologies, Slovak Gas Industry, Bratislava, Slovak Republic</ce:textfn></ce:affiliation><ce:affiliation id="AFF3"><ce:label>c</ce:label><ce:textfn>Faculty of Material Science and Technology, Slovak University of Technology, Bratislava, Slovak Republic</ce:textfn></ce:affiliation><ce:correspondence id="CORR1"><ce:label>*</ce:label><ce:text>Corresponding author. Tel.: +42-07-59410660; fax: +42-07-54775928</ce:text></ce:correspondence></ce:author-group><ce:date-received day="7" month="10" year="1999"></ce:date-received><ce:date-revised day="2" month="3" year="2000"></ce:date-revised><ce:date-accepted day="7" month="3" year="2000"></ce:date-accepted><ce:abstract><ce:section-title>Abstract</ce:section-title><ce:abstract-sec><ce:simple-para>The characteristics of specific binding of human [<ce:sup loc="pre">125</ce:sup>I]Tyr<ce:sup>13</ce:sup>-endothelin-(1–21), [<ce:sup loc="pre">125</ce:sup>I]-Tyr<ce:sup>13</ce:sup>-Suc-[Glu<ce:sup>9</ce:sup>,Ala<ce:sup>11,15</ce:sup>]-endothelin-(8–21), ([<ce:sup loc="pre">125</ce:sup>I]IRL-1620) and endothelin ET<ce:inf>A</ce:inf> receptor antagonist [<ce:sup loc="pre">125</ce:sup>I]Tyr<ce:sup>3</ce:sup>-(<ce:italic>N</ce:italic>-[(hexahydro-1<ce:italic>H</ce:italic>-azepin-1-yl)carbonyl]-<ce:small-caps>l</ce:small-caps>-Leu]-1Me)-<ce:small-caps>d</ce:small-caps>-Trp ([<ce:sup loc="pre">125</ce:sup>I]PD151242) (number of sites and their affinity) and proliferation responses to exogenous endothelin receptor agonists (endothelin-1 and the endothelin ET<ce:inf>B</ce:inf> receptor-selective, truncated <ce:italic>N</ce:italic>-acetyl-[Ala<ce:sup>11,15</ce:sup>]-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 ET<ce:inf>B</ce:inf> receptors and was much more intensive in tumorigenic cells. BQ3020, acting mostly through its C-terminus, induced nearly maximal endothelin ET<ce:inf>B</ce:inf> receptor down-regulation in HeLa cells. Staurosporine, a wide spectrum protein kinase inhibitor, significantly reduced, and <ce:italic>N</ce:italic>-[<ce:italic>N</ce:italic>-[<ce:italic>N</ce:italic>-[2,6-dimethyl-1piperidinyl)carbonyl]-4-Me-<ce:small-caps>l-</ce:small-caps>Leu]-1-(methoxycarbonyl)-<ce:small-caps>d</ce:small-caps>-tryptophanyl]-<ce:small-caps>d</ce:small-caps>-norleucine (BQ788), an endothelin ET<ce:inf>B</ce:inf> receptor antagonist, attenuated the down-regulation of endothelin receptors induced by endothelin receptor agonists. The down-regulation of endothelin ET<ce:inf>B</ce:inf> 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-<ce:small-caps>d</ce:small-caps>-10,11-dihydro-5<ce:italic>H</ce:italic>-dibenzo[<ce:italic>a</ce:italic>,<ce:italic>d</ce:italic>] cycloheptene-glycine-3,3-<ce:small-caps>d</ce:small-caps>-diphenyl-Ala-Leu-Asp-Ile-Ile-Trp (PD142893) and it was only partially reduced by the endothelin ET<ce:inf>A</ce:inf> receptor-selective endothelin antagonist PD151242.</ce:simple-para></ce:abstract-sec></ce:abstract><ce:keywords class="keyword"><ce:section-title>Keywords</ce:section-title><ce:keyword><ce:text>Endothelin ET<ce:inf>A</ce:inf> receptor</ce:text></ce:keyword><ce:keyword><ce:text>Endothelin ET<ce:inf>B</ce:inf> receptor</ce:text></ce:keyword><ce:keyword><ce:text>Fibroblast</ce:text></ce:keyword><ce:keyword><ce:text>(Human)</ce:text></ce:keyword><ce:keyword><ce:text>HeLa cell</ce:text></ce:keyword></ce:keywords></head></converted-article></istex:document></istex:metadataXml><mods version="3.6"><titleInfo><title>Enhanced endothelin ETB receptor down-regulation in human tumor cells</title></titleInfo><titleInfo type="alternative" contentType="CDATA"><title>Enhanced endothelin ET</title></titleInfo><name type="personal"><namePart type="given">Jan</namePart><namePart type="family">Drimal</namePart><affiliation>E-mail: exfadrim@savba.sk</affiliation><affiliation>Institute of Experimental Pharmacology, Cardiovascular Research Laboratory, Slovak Academy of Sciences, Dubravska cesta 9, 842 16 Bratislava, Slovak Republic</affiliation><description>Corresponding author. Tel.: +42-07-59410660; fax: +42-07-54775928</description><role><roleTerm type="text">author</roleTerm></role></name><name type="personal"><namePart type="given">Jan</namePart><namePart type="family">Drimal, Jr</namePart><affiliation>Department of Information Technologies, Slovak Gas Industry, Bratislava, Slovak Republic</affiliation><role><roleTerm type="text">author</roleTerm></role></name><name type="personal"><namePart type="given">Daniel</namePart><namePart type="family">Drimal</namePart><affiliation>Faculty of Material Science and Technology, Slovak University of Technology, Bratislava, Slovak Republic</affiliation><role><roleTerm type="text">author</roleTerm></role></name><typeOfResource>text</typeOfResource><genre type="brief-communication" displayLabel="Short communication" authority="ISTEX" authorityURI="https://content-type.data.istex.fr" valueURI="https://content-type.data.istex.fr/ark:/67375/XTP-S9SX2MFS-0">brief-communication</genre><originInfo><publisher>ELSEVIER</publisher><dateIssued encoding="w3cdtf">2000</dateIssued><dateModified encoding="w3cdtf">2000-03-02</dateModified><copyrightDate encoding="w3cdtf">2000</copyrightDate></originInfo><language><languageTerm type="code" authority="iso639-2b">eng</languageTerm><languageTerm type="code" authority="rfc3066">en</languageTerm></language><abstract 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.</abstract><note type="content">Section title: Short communication</note><note type="content">Table 1: The intensity of down-regulation of endothelin receptors on cultured normal and tumorigenic human cells With the nonselective human endothelin-1 and with the endothelin ETB receptor-selective, truncated endothelin-1-(6–21) analogue, linear peptide BQ3020. Characteristics of binding of radioactive ligands [125I]endothelin-1 with preferential affinity for endothelin ETA receptors (ETA≫ETB) and truncated (endothelin-1-(8–21) ligand [125I]IRL-1620, with preferential affinity for endothelin ETB receptors (ETB≫ETA). Measured parameters: (D) Surface endothelin receptor density; (A) Affinity, expressed here as Kd; and (P) Proliferative response ([3H]thymidine incorporation) are expressed as percentages of control. Values are Means±S.E.M., (n=24).</note><subject><genre>Keywords</genre><topic>Endothelin ETA receptor</topic><topic>Endothelin ETB receptor</topic><topic>Fibroblast</topic><topic>(Human)</topic><topic>HeLa cell</topic></subject><relatedItem type="host"><titleInfo><title>European Journal of Pharmacology</title></titleInfo><titleInfo type="abbreviated"><title>EJP</title></titleInfo><genre type="journal" authority="ISTEX" authorityURI="https://publication-type.data.istex.fr" valueURI="https://publication-type.data.istex.fr/ark:/67375/JMC-0GLKJH51-B">journal</genre><originInfo><publisher>ELSEVIER</publisher><dateIssued encoding="w3cdtf">2000</dateIssued></originInfo><identifier type="ISSN">0014-2999</identifier><identifier type="PII">S0014-2999(00)X0256-7</identifier><part><date>2000</date><detail type="volume"><number>396</number><caption>vol.</caption></detail><detail type="issue"><number>1</number><caption>no.</caption></detail><extent unit="issue-pages"><start>R1</start><end>R4</end></extent><extent unit="issue-pages"><start>1</start><end>52</end></extent><extent unit="pages"><start>19</start><end>22</end></extent></part></relatedItem><identifier type="istex">4E0E76FB81F50348B32F1CCECBC4B4C513F83127</identifier><identifier type="ark">ark:/67375/6H6-DHK4H0C7-6</identifier><identifier type="DOI">10.1016/S0014-2999(00)00198-9</identifier><identifier type="PII">S0014-2999(00)00198-9</identifier><accessCondition type="use and reproduction" contentType="copyright">©2000 Elsevier Science B.V.</accessCondition><recordInfo><recordContentSource authority="ISTEX" authorityURI="https://loaded-corpus.data.istex.fr" valueURI="https://loaded-corpus.data.istex.fr/ark:/67375/XBH-HKKZVM7B-M">elsevier</recordContentSource><recordOrigin>Elsevier Science B.V., ©2000</recordOrigin></recordInfo></mods><json:item><extension>json</extension><original>false</original><mimetype>application/json</mimetype><uri>https://api.istex.fr/ark:/67375/6H6-DHK4H0C7-6/record.json</uri></json:item></metadata><serie></serie></istex></record>Pour manipuler ce document sous Unix (Dilib)
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