Indium-111 labeling of low density lipoproteins with the DTPA-bis(stearylamide): evaluation as a potential radiopharmaceutical for tumor localization.
Identifieur interne : 007F29 ( Main/Exploration ); précédent : 007F28; suivant : 007F30Indium-111 labeling of low density lipoproteins with the DTPA-bis(stearylamide): evaluation as a potential radiopharmaceutical for tumor localization.
Auteurs : RBID : pubmed:8741993English descriptors
- KwdEn :
- Cell Line, Cell Membrane (metabolism), Chromatography, Gel, Drug Stability, Gadolinium DTPA, Humans, Indicators and Reagents, Indium Radioisotopes, Kinetics, Lipoproteins, LDL (diagnostic use), Lipoproteins, LDL (metabolism), Pentetic Acid (analogs & derivatives), Radioimmunodetection, Radioligand Assay, Receptors, LDL (metabolism), Stearates, Time Factors, Tumor Cells, Cultured.
- MESH :
- chemical , analogs & derivatives : Pentetic Acid.
- chemical , diagnostic use : Lipoproteins, LDL.
- chemical , metabolism : Lipoproteins, LDL, Receptors, LDL.
- chemical : Gadolinium DTPA, Indicators and Reagents, Indium Radioisotopes, Stearates.
- metabolism : Cell Membrane.
- Cell Line, Chromatography, Gel, Drug Stability, Humans, Kinetics, Radioimmunodetection, Radioligand Assay, Time Factors, Tumor Cells, Cultured.
Abstract
In order to use the LDL receptor pathway to target radionuclides to cancer sites for imaging and diagnostic purposes, a labeling procedure of LDL with 111In using the DTPA-bis(stearylamide) (L) has been developed. This bifunctional ligand is intended to be incorporated into the phospholipid monolayer of LDL and to specifically chelate the In3+ cation at the surface. The ligand was incorporated into LDL in buffered medium with a 65-80% yield. The L-LDL samples are stable over a 24 h period when examined by dialysis, allowing their storage before indium-111 radiolabeling. In vitro studies of In-L-LDL particles show that indium labeling is rapidly achieved (1 h). More than 85% of the indium atoms are bound to the chelating functions of the incorporated DTPA derivatives and less than 10% to the nonspecific complexation sites of LDL (e.g., protein residues). After incubation in human serum, the indium activity recovered in the LDL fraction of In-L-LDL samples (95%) is much higher than in In-LDL samples (35%), pointing out the strong stabilizing chelating effect of the ligand. Competitive binding studies show that In-L-LDL are recognized by LDL receptors of A549 cells like native LDL when the In-L/LDL ratio varies from 5 to 30. All these in vitro experiments demonstrate that the In-L-LDL conjugates possess properties suitable for further work with in vivo experiments.
DOI: 10.1021/bc950073l
PubMed: 8741993
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Indium-111 labeling of low density lipoproteins with the DTPA-bis(stearylamide): evaluation as a potential radiopharmaceutical for tumor localization.</title><author><name sortKey="Jasanada, F" uniqKey="Jasanada F">F Jasanada</name><affiliation wicri:level="1"><nlm:affiliation>Faculté de Pharmacie, Université Paul Sabatier, Toulouse, France.</nlm:affiliation><country xml:lang="fr">France</country><wicri:regionArea>Faculté de Pharmacie, Université Paul Sabatier, Toulouse</wicri:regionArea><placeName><region type="région">Midi-Pyrénées</region><settlement type="city">Toulouse</settlement></placeName></affiliation></author><author><name sortKey="Urizzi, P" uniqKey="Urizzi P">P Urizzi</name></author><author><name sortKey="Souchard, J P" uniqKey="Souchard J">J P Souchard</name></author><author><name sortKey="Le Gaillard, F" uniqKey="Le Gaillard F">F Le Gaillard</name></author><author><name sortKey="Favre, G" uniqKey="Favre G">G Favre</name></author><author><name sortKey="Nepveu, F" uniqKey="Nepveu F">F Nepveu</name></author></titleStmt><publicationStmt><date when="????"><PubDate><MedlineDate>1996 Jan-Feb</MedlineDate></PubDate></date><idno type="RBID">pubmed:8741993</idno><idno type="pmid">8741993</idno><idno type="doi">10.1021/bc950073l</idno><idno type="wicri:Area/Main/Corpus">004789</idno><idno type="wicri:Area/Main/Curation">004789</idno><idno type="wicri:Area/Main/Exploration">007F29</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Cell Line</term><term>Cell Membrane (metabolism)</term><term>Chromatography, Gel</term><term>Drug Stability</term><term>Gadolinium DTPA</term><term>Humans</term><term>Indicators and Reagents</term><term>Indium Radioisotopes</term><term>Kinetics</term><term>Lipoproteins, LDL (diagnostic use)</term><term>Lipoproteins, LDL (metabolism)</term><term>Pentetic Acid (analogs & derivatives)</term><term>Radioimmunodetection</term><term>Radioligand Assay</term><term>Receptors, LDL (metabolism)</term><term>Stearates</term><term>Time Factors</term><term>Tumor Cells, Cultured</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Pentetic Acid</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Lipoproteins, LDL</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Lipoproteins, LDL</term><term>Receptors, LDL</term></keywords><keywords scheme="MESH" type="chemical" xml:lang="en"><term>Gadolinium DTPA</term><term>Indicators and Reagents</term><term>Indium Radioisotopes</term><term>Stearates</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Cell Membrane</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line</term><term>Chromatography, Gel</term><term>Drug Stability</term><term>Humans</term><term>Kinetics</term><term>Radioimmunodetection</term><term>Radioligand Assay</term><term>Time Factors</term><term>Tumor Cells, Cultured</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">In order to use the LDL receptor pathway to target radionuclides to cancer sites for imaging and diagnostic purposes, a labeling procedure of LDL with 111In using the DTPA-bis(stearylamide) (L) has been developed. This bifunctional ligand is intended to be incorporated into the phospholipid monolayer of LDL and to specifically chelate the In3+ cation at the surface. The ligand was incorporated into LDL in buffered medium with a 65-80% yield. The L-LDL samples are stable over a 24 h period when examined by dialysis, allowing their storage before indium-111 radiolabeling. In vitro studies of In-L-LDL particles show that indium labeling is rapidly achieved (1 h). More than 85% of the indium atoms are bound to the chelating functions of the incorporated DTPA derivatives and less than 10% to the nonspecific complexation sites of LDL (e.g., protein residues). After incubation in human serum, the indium activity recovered in the LDL fraction of In-L-LDL samples (95%) is much higher than in In-LDL samples (35%), pointing out the strong stabilizing chelating effect of the ligand. Competitive binding studies show that In-L-LDL are recognized by LDL receptors of A549 cells like native LDL when the In-L/LDL ratio varies from 5 to 30. All these in vitro experiments demonstrate that the In-L-LDL conjugates possess properties suitable for further work with in vivo experiments.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">8741993</PMID><DateCreated><Year>1996</Year><Month>10</Month><Day>11</Day></DateCreated><DateCompleted><Year>1996</Year><Month>10</Month><Day>11</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Print">1043-1802</ISSN><JournalIssue CitedMedium="Print"><Volume>7</Volume><Issue>1</Issue><PubDate><MedlineDate>1996 Jan-Feb</MedlineDate></PubDate></JournalIssue><Title>Bioconjugate chemistry</Title><ISOAbbreviation>Bioconjug. Chem.</ISOAbbreviation></Journal><ArticleTitle>Indium-111 labeling of low density lipoproteins with the DTPA-bis(stearylamide): evaluation as a potential radiopharmaceutical for tumor localization.</ArticleTitle><Pagination><MedlinePgn>72-81</MedlinePgn></Pagination><Abstract><AbstractText>In order to use the LDL receptor pathway to target radionuclides to cancer sites for imaging and diagnostic purposes, a labeling procedure of LDL with 111In using the DTPA-bis(stearylamide) (L) has been developed. This bifunctional ligand is intended to be incorporated into the phospholipid monolayer of LDL and to specifically chelate the In3+ cation at the surface. The ligand was incorporated into LDL in buffered medium with a 65-80% yield. The L-LDL samples are stable over a 24 h period when examined by dialysis, allowing their storage before indium-111 radiolabeling. In vitro studies of In-L-LDL particles show that indium labeling is rapidly achieved (1 h). More than 85% of the indium atoms are bound to the chelating functions of the incorporated DTPA derivatives and less than 10% to the nonspecific complexation sites of LDL (e.g., protein residues). After incubation in human serum, the indium activity recovered in the LDL fraction of In-L-LDL samples (95%) is much higher than in In-LDL samples (35%), pointing out the strong stabilizing chelating effect of the ligand. Competitive binding studies show that In-L-LDL are recognized by LDL receptors of A549 cells like native LDL when the In-L/LDL ratio varies from 5 to 30. All these in vitro experiments demonstrate that the In-L-LDL conjugates possess properties suitable for further work with in vivo experiments.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Jasanada</LastName><ForeName>F</ForeName><Initials>F</Initials><Affiliation>Faculté de Pharmacie, Université Paul Sabatier, Toulouse, France.</Affiliation></Author><Author ValidYN="Y"><LastName>Urizzi</LastName><ForeName>P</ForeName><Initials>P</Initials></Author><Author ValidYN="Y"><LastName>Souchard</LastName><ForeName>J P</ForeName><Initials>JP</Initials></Author><Author ValidYN="Y"><LastName>Le Gaillard</LastName><ForeName>F</ForeName><Initials>F</Initials></Author><Author ValidYN="Y"><LastName>Favre</LastName><ForeName>G</ForeName><Initials>G</Initials></Author><Author ValidYN="Y"><LastName>Nepveu</LastName><ForeName>F</ForeName><Initials>F</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList></Article><MedlineJournalInfo><Country>UNITED STATES</Country><MedlineTA>Bioconjug Chem</MedlineTA><NlmUniqueID>9010319</NlmUniqueID><ISSNLinking>1043-1802</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indicators and Reagents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Lipoproteins, LDL</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, LDL</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Stearates</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>gadolinium stearylamide DTPA</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>indium DTPA-bis(stearylamide)</NameOfSubstance></Chemical><Chemical><RegistryNumber>7A314HQM0I</RegistryNumber><NameOfSubstance>Pentetic Acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>K2I13DR72L</RegistryNumber><NameOfSubstance>Gadolinium DTPA</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Cell Line</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cell Membrane</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Chromatography, Gel</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Stability</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Gadolinium DTPA</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indicators and Reagents</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Indium Radioisotopes</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Kinetics</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lipoproteins, LDL</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Pentetic Acid</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radioimmunodetection</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radioligand Assay</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, LDL</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Stearates</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Time Factors</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tumor Cells, Cultured</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="pubmed"><Year>1996</Year><Month>1</Month><Day>1</Day></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>1996</Year><Month>1</Month><Day>1</Day><Hour>0</Hour><Minute>1</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>1996</Year><Month>1</Month><Day>1</Day><Hour>0</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">8741993</ArticleId><ArticleId IdType="doi">10.1021/bc950073l</ArticleId><ArticleId IdType="pii">bc950073l</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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