Characterization of ligand binding and processing by gastrin-releasing peptide receptors in a small-cell lung cancer cell line.
Identifieur interne : 002E23 ( Main/Exploration ); précédent : 002E22; suivant : 002E24Characterization of ligand binding and processing by gastrin-releasing peptide receptors in a small-cell lung cancer cell line.
Auteurs : C. Cardona [Royaume-Uni] ; N M Bleehen ; J G ReeveSource :
- The Biochemical journal [ 0264-6021 ] ; 1992.
Descripteurs français
- KwdFr :
- Antibactériens (pharmacologie), Bombésine (métabolisme), Carcinome à petites cellules, Chloroquine (pharmacologie), Cinétique, Fixation compétitive, Glycopeptides (pharmacologie), Humains, Ligands, Lignée cellulaire, Peptide libérant la gastrine, Peptides (), Peptides (métabolisme), Récepteur bombésine, Récepteurs aux neuromédiateurs (métabolisme), Tumeurs du poumon.
- MESH :
- métabolisme : Bombésine, Peptides, Récepteurs aux neuromédiateurs.
- pharmacologie : Antibactériens, Chloroquine, Glycopeptides.
- Carcinome à petites cellules, Cinétique, Fixation compétitive, Humains, Ligands, Lignée cellulaire, Peptide libérant la gastrine, Peptides, Récepteur bombésine, Tumeurs du poumon.
English descriptors
- KwdEn :
- Anti-Bacterial Agents (pharmacology), Binding, Competitive, Bombesin (metabolism), Carcinoma, Small Cell, Cell Line, Chloroquine (pharmacology), Gastrin-Releasing Peptide, Glycopeptides (pharmacology), Humans, Kinetics, Ligands, Lung Neoplasms, Peptides (drug effects), Peptides (metabolism), Receptors, Bombesin, Receptors, Neurotransmitter (metabolism).
- MESH :
- chemical , drug effects : Peptides.
- chemical , metabolism : Bombesin, Peptides, Receptors, Neurotransmitter.
- chemical , pharmacology : Anti-Bacterial Agents, Chloroquine, Glycopeptides.
- Binding, Competitive, Carcinoma, Small Cell, Cell Line, Gastrin-Releasing Peptide, Humans, Kinetics, Ligands, Lung Neoplasms, Receptors, Bombesin.
Abstract
The ligand-binding properties of the gastrin-releasing peptide (GRP) receptor and the cellular processing of GRP have been studied in the small-cell lung cancer (SCLC) cell line COR-L42. Scatchard analysis of GRP receptor expression indicated a single class of high-affinity receptors (Kd 1.5 nM) and approx. 6700 receptors/cell. GRP bound to its receptor with a Ki of 2.4 nM. The bombesin-related peptides neuromedin B (NMB) and phyllolitorin also bound to GRP receptors with Ki values of 22.7 and 59.1 nM respectively. Binding of 125I-GRP to COR-L42 cells increased rapidly at 37 degrees, achieved a maximum at 10 min and declined rapidly thereafter. At 4 degrees C, maximum binding was achieved at 30 min and the subsequent decline in cell-associated radioactivity was slower than that seen at 37 degrees C. Acid/salt extraction, to separate surface-bound ligand from internalized GRP, indicated that after receptor binding 125I-GRP was rapidly internalized. To determine the pathway of 125I-GRP degradation, binding studies were carried out with the lysosomotropic agent chloroquine (5 mM), and with phosphoramidon (10 microM), an inhibitor of the membrane-bound enzyme (EC 3.4.24.11). Both agents markedly inhibited the degradation of GRP, indicating that this process involves a lysosomal pathway and a phosphoramidon-sensitive pathway, possibly involving the EC 3.4.24.11 enzyme. GRP receptor down-regulation was observed following a 10 min exposure to 100 nM-GRP. With longer pretreatment times the number of binding sites recovered to 80% of control values. Treatment with 5 mM-chloroquine plus GRP or cycloheximide (10 micrograms/ml) plus GRP demonstrated that the majority of GRP receptors are recycled. NMB and phyllolitorin pretreatment did not influence the subsequent binding of 125I-GRP, suggesting that these peptides do not down-regulate GRP receptors.
DOI: 10.1042/bj2810115
PubMed: 1310003
Affiliations:
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Cardona</name><affiliation wicri:level="1"><nlm:affiliation>Clinical Oncology and Radiotherapeutics Unit, Medical Research Council, Cambridge, U.K.</nlm:affiliation><country xml:lang="fr">Royaume-Uni</country><wicri:regionArea>Clinical Oncology and Radiotherapeutics Unit, Medical Research Council, Cambridge</wicri:regionArea><wicri:noRegion>Cambridge</wicri:noRegion></affiliation></author><author><name sortKey="Bleehen, N M" sort="Bleehen, N M" uniqKey="Bleehen N" first="N M" last="Bleehen">N M Bleehen</name></author><author><name sortKey="Reeve, J G" sort="Reeve, J G" uniqKey="Reeve J" first="J G" last="Reeve">J G Reeve</name></author></titleStmt><publicationStmt><idno type="wicri:source">PubMed</idno><date when="1992">1992</date><idno type="RBID">pubmed:1310003</idno><idno type="pmid">1310003</idno><idno type="doi">10.1042/bj2810115</idno><idno type="wicri:Area/PubMed/Corpus">000549</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Corpus" wicri:corpus="PubMed">000549</idno><idno type="wicri:Area/PubMed/Curation">000549</idno><idno type="wicri:explorRef" wicri:stream="PubMed" wicri:step="Curation">000549</idno><idno type="wicri:Area/PubMed/Checkpoint">000524</idno><idno type="wicri:explorRef" wicri:stream="Checkpoint" wicri:step="PubMed">000524</idno><idno type="wicri:Area/Ncbi/Merge">000039</idno><idno type="wicri:Area/Ncbi/Curation">000039</idno><idno type="wicri:Area/Ncbi/Checkpoint">000039</idno><idno type="wicri:doubleKey">0264-6021:1992:Cardona C:characterization:of:ligand</idno><idno type="wicri:Area/Main/Merge">002E89</idno><idno type="wicri:Area/Main/Curation">002E23</idno><idno type="wicri:Area/Main/Exploration">002E23</idno></publicationStmt><sourceDesc><biblStruct><analytic><title xml:lang="en">Characterization of ligand binding and processing by gastrin-releasing peptide receptors in a small-cell lung cancer cell line.</title><author><name sortKey="Cardona, C" sort="Cardona, C" uniqKey="Cardona C" first="C" last="Cardona">C. Cardona</name><affiliation wicri:level="1"><nlm:affiliation>Clinical Oncology and Radiotherapeutics Unit, Medical Research Council, Cambridge, U.K.</nlm:affiliation><country xml:lang="fr">Royaume-Uni</country><wicri:regionArea>Clinical Oncology and Radiotherapeutics Unit, Medical Research Council, Cambridge</wicri:regionArea><wicri:noRegion>Cambridge</wicri:noRegion></affiliation></author><author><name sortKey="Bleehen, N M" sort="Bleehen, N M" uniqKey="Bleehen N" first="N M" last="Bleehen">N M Bleehen</name></author><author><name sortKey="Reeve, J G" sort="Reeve, J G" uniqKey="Reeve J" first="J G" last="Reeve">J G Reeve</name></author></analytic><series><title level="j">The Biochemical journal</title><idno type="ISSN">0264-6021</idno><imprint><date when="1992" type="published">1992</date></imprint></series></biblStruct></sourceDesc></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Anti-Bacterial Agents (pharmacology)</term><term>Binding, Competitive</term><term>Bombesin (metabolism)</term><term>Carcinoma, Small Cell</term><term>Cell Line</term><term>Chloroquine (pharmacology)</term><term>Gastrin-Releasing Peptide</term><term>Glycopeptides (pharmacology)</term><term>Humans</term><term>Kinetics</term><term>Ligands</term><term>Lung Neoplasms</term><term>Peptides (drug effects)</term><term>Peptides (metabolism)</term><term>Receptors, Bombesin</term><term>Receptors, Neurotransmitter (metabolism)</term></keywords><keywords scheme="KwdFr" xml:lang="fr"><term>Antibactériens (pharmacologie)</term><term>Bombésine (métabolisme)</term><term>Carcinome à petites cellules</term><term>Chloroquine (pharmacologie)</term><term>Cinétique</term><term>Fixation compétitive</term><term>Glycopeptides (pharmacologie)</term><term>Humains</term><term>Ligands</term><term>Lignée cellulaire</term><term>Peptide libérant la gastrine</term><term>Peptides ()</term><term>Peptides (métabolisme)</term><term>Récepteur bombésine</term><term>Récepteurs aux neuromédiateurs (métabolisme)</term><term>Tumeurs du poumon</term></keywords><keywords scheme="MESH" type="chemical" qualifier="drug effects" xml:lang="en"><term>Peptides</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Bombesin</term><term>Peptides</term><term>Receptors, Neurotransmitter</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Anti-Bacterial Agents</term><term>Chloroquine</term><term>Glycopeptides</term></keywords><keywords scheme="MESH" qualifier="métabolisme" xml:lang="fr"><term>Bombésine</term><term>Peptides</term><term>Récepteurs aux neuromédiateurs</term></keywords><keywords scheme="MESH" qualifier="pharmacologie" xml:lang="fr"><term>Antibactériens</term><term>Chloroquine</term><term>Glycopeptides</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Binding, Competitive</term><term>Carcinoma, Small Cell</term><term>Cell Line</term><term>Gastrin-Releasing Peptide</term><term>Humans</term><term>Kinetics</term><term>Ligands</term><term>Lung Neoplasms</term><term>Receptors, Bombesin</term></keywords><keywords scheme="MESH" xml:lang="fr"><term>Carcinome à petites cellules</term><term>Cinétique</term><term>Fixation compétitive</term><term>Humains</term><term>Ligands</term><term>Lignée cellulaire</term><term>Peptide libérant la gastrine</term><term>Peptides</term><term>Récepteur bombésine</term><term>Tumeurs du poumon</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The ligand-binding properties of the gastrin-releasing peptide (GRP) receptor and the cellular processing of GRP have been studied in the small-cell lung cancer (SCLC) cell line COR-L42. Scatchard analysis of GRP receptor expression indicated a single class of high-affinity receptors (Kd 1.5 nM) and approx. 6700 receptors/cell. GRP bound to its receptor with a Ki of 2.4 nM. The bombesin-related peptides neuromedin B (NMB) and phyllolitorin also bound to GRP receptors with Ki values of 22.7 and 59.1 nM respectively. Binding of 125I-GRP to COR-L42 cells increased rapidly at 37 degrees, achieved a maximum at 10 min and declined rapidly thereafter. At 4 degrees C, maximum binding was achieved at 30 min and the subsequent decline in cell-associated radioactivity was slower than that seen at 37 degrees C. Acid/salt extraction, to separate surface-bound ligand from internalized GRP, indicated that after receptor binding 125I-GRP was rapidly internalized. To determine the pathway of 125I-GRP degradation, binding studies were carried out with the lysosomotropic agent chloroquine (5 mM), and with phosphoramidon (10 microM), an inhibitor of the membrane-bound enzyme (EC 3.4.24.11). Both agents markedly inhibited the degradation of GRP, indicating that this process involves a lysosomal pathway and a phosphoramidon-sensitive pathway, possibly involving the EC 3.4.24.11 enzyme. GRP receptor down-regulation was observed following a 10 min exposure to 100 nM-GRP. With longer pretreatment times the number of binding sites recovered to 80% of control values. Treatment with 5 mM-chloroquine plus GRP or cycloheximide (10 micrograms/ml) plus GRP demonstrated that the majority of GRP receptors are recycled. NMB and phyllolitorin pretreatment did not influence the subsequent binding of 125I-GRP, suggesting that these peptides do not down-regulate GRP receptors.</div></front></TEI><affiliations><list><country><li>Royaume-Uni</li></country></list><tree><noCountry><name sortKey="Bleehen, N M" sort="Bleehen, N M" uniqKey="Bleehen N" first="N M" last="Bleehen">N M Bleehen</name><name sortKey="Reeve, J G" sort="Reeve, J G" uniqKey="Reeve J" first="J G" last="Reeve">J G Reeve</name></noCountry><country name="Royaume-Uni"><noRegion><name sortKey="Cardona, C" sort="Cardona, C" uniqKey="Cardona C" first="C" last="Cardona">C. Cardona</name></noRegion></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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