Influence of chelate conjugation on a newly identified tumor-targeting peptide.
Identifieur interne : 002661 ( Main/Exploration ); précédent : 002660; suivant : 002662Influence of chelate conjugation on a newly identified tumor-targeting peptide.
Auteurs : RBID : pubmed:17704241English descriptors
- KwdEn :
- Animals, Binding, Competitive, Cell Line, Tumor, Chelating Agents (chemistry), Female, Heterocyclic Compounds, 1-Ring (chemical synthesis), Heterocyclic Compounds, 1-Ring (chemistry), Heterocyclic Compounds, 1-Ring (pharmacokinetics), Humans, Indium Radioisotopes, Mice, Mice, Nude, Neoplasm Transplantation, Oligopeptides (chemistry), Peptides (chemical synthesis), Peptides (chemistry), Peptides (pharmacokinetics), Radiopharmaceuticals (chemical synthesis), Radiopharmaceuticals (chemistry), Radiopharmaceuticals (pharmacokinetics), Tissue Distribution, Transplantation, Heterologous.
- MESH :
- chemical , chemical synthesis : Heterocyclic Compounds, 1-Ring, Peptides, Radiopharmaceuticals.
- chemical , chemistry : Chelating Agents, Heterocyclic Compounds, 1-Ring, Oligopeptides, Peptides, Radiopharmaceuticals.
- chemical , pharmacokinetics : Heterocyclic Compounds, 1-Ring, Peptides, Radiopharmaceuticals.
- Animals, Binding, Competitive, Cell Line, Tumor, Female, Humans, Indium Radioisotopes, Mice, Mice, Nude, Neoplasm Transplantation, Tissue Distribution, Transplantation, Heterologous.
Abstract
The transfer of peptide sequences identified by screening of phage-displayed libraries to clinical application is often difficult. This study investigated whether coupling of a new peptide, FROP-1, to the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) resulted in structural restriction and, consequently, improved binding and stability.
DOI: 10.2967/jnumed.106.036707
PubMed: 17704241
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Influence of chelate conjugation on a newly identified tumor-targeting peptide.</title><author><name sortKey="Mier, Walter" uniqKey="Mier W">Walter Mier</name><affiliation wicri:level="3"><nlm:affiliation>Department of Nuclear Medicine, University of Heidelberg, Heidelberg, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>Department of Nuclear Medicine, University of Heidelberg, Heidelberg</wicri:regionArea><placeName><region type="land" nuts="1">Bade-Wurtemberg</region><region type="district" nuts="2">District de Karlsruhe</region><settlement type="city">Heidelberg</settlement></placeName></affiliation></author><author><name sortKey="Zitzmann, Sabine" uniqKey="Zitzmann S">Sabine Zitzmann</name></author><author><name sortKey="Kr Mer, Susanne" uniqKey="Kr Mer S">Susanne Krämer</name></author><author><name sortKey="Reed, Jennifer" uniqKey="Reed J">Jennifer Reed</name></author><author><name sortKey="Knapp, Eva Maria" uniqKey="Knapp E">Eva-Maria Knapp</name></author><author><name sortKey="Altmann, Annette" uniqKey="Altmann A">Annette Altmann</name></author><author><name sortKey="Eisenhut, Michael" uniqKey="Eisenhut M">Michael Eisenhut</name></author><author><name sortKey="Haberkorn, Uwe" uniqKey="Haberkorn U">Uwe Haberkorn</name></author></titleStmt><publicationStmt><date when="2007">2007</date><idno type="doi">10.2967/jnumed.106.036707</idno><idno type="RBID">pubmed:17704241</idno><idno type="pmid">17704241</idno><idno type="wicri:Area/Main/Corpus">002703</idno><idno type="wicri:Area/Main/Curation">002703</idno><idno type="wicri:Area/Main/Exploration">002661</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Binding, Competitive</term><term>Cell Line, Tumor</term><term>Chelating Agents (chemistry)</term><term>Female</term><term>Heterocyclic Compounds, 1-Ring (chemical synthesis)</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (pharmacokinetics)</term><term>Humans</term><term>Indium Radioisotopes</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term><term>Oligopeptides (chemistry)</term><term>Peptides (chemical synthesis)</term><term>Peptides (chemistry)</term><term>Peptides (pharmacokinetics)</term><term>Radiopharmaceuticals (chemical synthesis)</term><term>Radiopharmaceuticals (chemistry)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Tissue Distribution</term><term>Transplantation, Heterologous</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Peptides</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Chelating Agents</term><term>Heterocyclic Compounds, 1-Ring</term><term>Oligopeptides</term><term>Peptides</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Peptides</term><term>Radiopharmaceuticals</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Binding, Competitive</term><term>Cell Line, Tumor</term><term>Female</term><term>Humans</term><term>Indium Radioisotopes</term><term>Mice</term><term>Mice, Nude</term><term>Neoplasm Transplantation</term><term>Tissue Distribution</term><term>Transplantation, Heterologous</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The transfer of peptide sequences identified by screening of phage-displayed libraries to clinical application is often difficult. This study investigated whether coupling of a new peptide, FROP-1, to the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) resulted in structural restriction and, consequently, improved binding and stability.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">17704241</PMID><DateCreated><Year>2007</Year><Month>09</Month><Day>05</Day></DateCreated><DateCompleted><Year>2007</Year><Month>11</Month><Day>27</Day></DateCompleted><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Print">0161-5505</ISSN><JournalIssue CitedMedium="Print"><Volume>48</Volume><Issue>9</Issue><PubDate><Year>2007</Year><Month>Sep</Month></PubDate></JournalIssue><Title>Journal of nuclear medicine : official publication, Society of Nuclear Medicine</Title><ISOAbbreviation>J. Nucl. Med.</ISOAbbreviation></Journal><ArticleTitle>Influence of chelate conjugation on a newly identified tumor-targeting peptide.</ArticleTitle><Pagination><MedlinePgn>1545-52</MedlinePgn></Pagination><Abstract><AbstractText Label="UNLABELLED">The transfer of peptide sequences identified by screening of phage-displayed libraries to clinical application is often difficult. This study investigated whether coupling of a new peptide, FROP-1, to the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) resulted in structural restriction and, consequently, improved binding and stability.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">The peptide FROP-1 was coupled to the chelator DOTA and labeled with (111)In. The structural changes caused by the addition of the chelator were determined by circular dichroism. The properties of this modified peptide were investigated in in vitro binding assays and monitored for kinetics, competition, and internalization as well as serum stability. A cell-type binding profile was established and the in vivo biodistribution was evaluated in a nude mouse model.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">When compared with the free peptide without chelator, FROPDOTA revealed different cellular uptake kinetics, reaching a maximum at 2 h in vitro. The cells completely accumulated the tracer, and competition experiments revealed that 99.4% (FRO82-2 cells), 98.6% (MCF-7 cells), or 99.3% (average for 3 primary head and neck tumor cell lines) of tracer accumulation could be suppressed, revealing the specificity of this process. The internalization kinetics determined in MCF-7 cells supported this finding: After an incubation time of 180 min, the major fraction of FROPDOTA was trapped intracellularly. Serum stability experiments revealed an increase in stability due to the chelator, with a half-life of 71 min. Circular dichroism measurements indicated a fixed alpha-helix structure of FROPDOTA representing a strong change in secondary structure. In competition binding experiments, the binding constant (K(D)) to FRO82-2 cells was determined to be 494 nM. Despite this avid binding affinity, the binding kinetics were found to be too slow to induce an uptake in vivo before clearance. Consequently, the biodistribution revealed a rapid renal and hepatobiliary clearance, with blood levels dropping from 5.48 +/- 0.26 %ID/g (percentage injected dose per gram) 5 min after injection to 0.77 +/- 0.15 %ID/g at 135 min after injection.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">This study revealed that peptides that are identified by display techniques may be underrated. Careful alteration of their structure will permit going beyond the possibilities that the limited pool of naturally occurring peptides provide for tumor targeting.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Mier</LastName><ForeName>Walter</ForeName><Initials>W</Initials><Affiliation>Department of Nuclear Medicine, University of Heidelberg, Heidelberg, Germany.</Affiliation></Author><Author ValidYN="Y"><LastName>Zitzmann</LastName><ForeName>Sabine</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Krämer</LastName><ForeName>Susanne</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Reed</LastName><ForeName>Jennifer</ForeName><Initials>J</Initials></Author><Author ValidYN="Y"><LastName>Knapp</LastName><ForeName>Eva-Maria</ForeName><Initials>EM</Initials></Author><Author ValidYN="Y"><LastName>Altmann</LastName><ForeName>Annette</ForeName><Initials>A</Initials></Author><Author ValidYN="Y"><LastName>Eisenhut</LastName><ForeName>Michael</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Haberkorn</LastName><ForeName>Uwe</ForeName><Initials>U</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2007</Year><Month>08</Month><Day>17</Day></ArticleDate></Article><MedlineJournalInfo><Country>United States</Country><MedlineTA>J Nucl Med</MedlineTA><NlmUniqueID>0217410</NlmUniqueID><ISSNLinking>0161-5505</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Chelating Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>FROP-1 peptide</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>FROPDOTA compound</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Heterocyclic Compounds, 1-Ring</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Oligopeptides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Peptides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>60239-18-1</RegistryNumber><NameOfSubstance>1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Binding, Competitive</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Chelating Agents</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName MajorTopicYN="Y">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Indium Radioisotopes</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasm Transplantation</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Oligopeptides</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Peptides</DescriptorName><QualifierName MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Transplantation, Heterologous</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="aheadofprint"><Year>2007</Year><Month>8</Month><Day>17</Day></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2007</Year><Month>8</Month><Day>21</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2007</Year><Month>12</Month><Day>6</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2007</Year><Month>8</Month><Day>21</Day><Hour>9</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pii">jnumed.106.036707</ArticleId><ArticleId IdType="doi">10.2967/jnumed.106.036707</ArticleId><ArticleId IdType="pubmed">17704241</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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