Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.
Identifieur interne : 000B28 ( Main/Exploration ); précédent : 000B27; suivant : 000B29Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.
Auteurs : RBID : pubmed:21732165English descriptors
- KwdEn :
- Animals, Cell Line, Tumor, Drug Evaluation, Preclinical, Female, Gallium Radioisotopes, Gastrins (chemistry), Gastrins (pharmacokinetics), Heterocyclic Compounds, 1-Ring (chemistry), Heterocyclic Compounds, 1-Ring (pharmacokinetics), Indium Radioisotopes, Mice, Mice, Inbred BALB C, Mice, Nude, Mice, SCID, Receptors, Cholecystokinin (metabolism), Thyroid Neoplasms (metabolism), Thyroid Neoplasms (radionuclide imaging), Tomography, Emission-Computed, Single-Photon (methods).
- MESH :
- chemical , chemistry : Gastrins, Heterocyclic Compounds, 1-Ring.
- chemical , metabolism : Receptors, Cholecystokinin.
- chemical , pharmacokinetics : Gastrins, Heterocyclic Compounds, 1-Ring.
- chemical : Gallium Radioisotopes, Indium Radioisotopes.
- metabolism : Thyroid Neoplasms.
- methods : Tomography, Emission-Computed, Single-Photon.
- radionuclide imaging : Thyroid Neoplasms.
- Animals, Cell Line, Tumor, Drug Evaluation, Preclinical, Female, Mice, Mice, Inbred BALB C, Mice, Nude, Mice, SCID.
Abstract
Targeting of cholecystokinin receptor expressing malignancies such as medullary thyroid carcinoma is currently limited by low in vivo stability of radioligands. To increase the stability, we have developed and preclinically evaluated two cyclic 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-minigastrin analogs radiolabeled with (111)In and (68)Ga.
DOI: 10.1007/s11307-011-0506-2
PubMed: 21732165
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.</title><author><name sortKey="Von Guggenberg, Elisabeth" uniqKey="Von Guggenberg E">Elisabeth von Guggenberg</name><affiliation wicri:level="1"><nlm:affiliation>Department of Nuclear Medicine, Innsbruck Medical University, Anichstrasse 35, 6020, Innsbruck, Austria. elisabeth.vonguggenberg@uki.at</nlm:affiliation><country xml:lang="fr">Autriche</country><wicri:regionArea>Department of Nuclear Medicine, Innsbruck Medical University, Anichstrasse 35, 6020, Innsbruck</wicri:regionArea></affiliation></author><author><name sortKey="Rangger, Christine" uniqKey="Rangger C">Christine Rangger</name></author><author><name sortKey="Sosabowski, Jane" uniqKey="Sosabowski J">Jane Sosabowski</name></author><author><name sortKey="Laverman, Peter" uniqKey="Laverman P">Peter Laverman</name></author><author><name sortKey="Reubi, Jean Claude" uniqKey="Reubi J">Jean-Claude Reubi</name></author><author><name sortKey="Virgolini, Irene Johanna" uniqKey="Virgolini I">Irene Johanna Virgolini</name></author><author><name sortKey="Decristoforo, Clemens" uniqKey="Decristoforo C">Clemens Decristoforo</name></author></titleStmt><publicationStmt><date when="2012">2012</date><idno type="doi">10.1007/s11307-011-0506-2</idno><idno type="RBID">pubmed:21732165</idno><idno type="pmid">21732165</idno><idno type="wicri:Area/Main/Corpus">001288</idno><idno type="wicri:Area/Main/Curation">001288</idno><idno type="wicri:Area/Main/Exploration">000B28</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Drug Evaluation, Preclinical</term><term>Female</term><term>Gallium Radioisotopes</term><term>Gastrins (chemistry)</term><term>Gastrins (pharmacokinetics)</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (pharmacokinetics)</term><term>Indium Radioisotopes</term><term>Mice</term><term>Mice, Inbred BALB C</term><term>Mice, Nude</term><term>Mice, SCID</term><term>Receptors, Cholecystokinin (metabolism)</term><term>Thyroid Neoplasms (metabolism)</term><term>Thyroid Neoplasms (radionuclide imaging)</term><term>Tomography, Emission-Computed, Single-Photon (methods)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Gastrins</term><term>Heterocyclic Compounds, 1-Ring</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Receptors, Cholecystokinin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Gastrins</term><term>Heterocyclic Compounds, 1-Ring</term></keywords><keywords scheme="MESH" type="chemical" xml:lang="en"><term>Gallium Radioisotopes</term><term>Indium Radioisotopes</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Thyroid Neoplasms</term></keywords><keywords scheme="MESH" qualifier="methods" xml:lang="en"><term>Tomography, Emission-Computed, Single-Photon</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Thyroid Neoplasms</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Drug Evaluation, Preclinical</term><term>Female</term><term>Mice</term><term>Mice, Inbred BALB C</term><term>Mice, Nude</term><term>Mice, SCID</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Targeting of cholecystokinin receptor expressing malignancies such as medullary thyroid carcinoma is currently limited by low in vivo stability of radioligands. To increase the stability, we have developed and preclinically evaluated two cyclic 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-minigastrin analogs radiolabeled with (111)In and (68)Ga.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">21732165</PMID><DateCreated><Year>2012</Year><Month>05</Month><Day>08</Day></DateCreated><DateCompleted><Year>2012</Year><Month>10</Month><Day>29</Day></DateCompleted><Article PubModel="Print"><Journal><ISSN IssnType="Electronic">1860-2002</ISSN><JournalIssue CitedMedium="Internet"><Volume>14</Volume><Issue>3</Issue><PubDate><Year>2012</Year><Month>Jun</Month></PubDate></JournalIssue><Title>Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging</Title><ISOAbbreviation>Mol Imaging Biol</ISOAbbreviation></Journal><ArticleTitle>Preclinical evaluation of radiolabeled DOTA-derivatized cyclic minigastrin analogs for targeting cholecystokinin receptor expressing malignancies.</ArticleTitle><Pagination><MedlinePgn>366-75</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1007/s11307-011-0506-2</ELocationID><Abstract><AbstractText Label="PURPOSE" NlmCategory="OBJECTIVE">Targeting of cholecystokinin receptor expressing malignancies such as medullary thyroid carcinoma is currently limited by low in vivo stability of radioligands. To increase the stability, we have developed and preclinically evaluated two cyclic 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-minigastrin analogs radiolabeled with (111)In and (68)Ga.</AbstractText><AbstractText Label="PROCEDURES" NlmCategory="METHODS">Radiolabeling efficiency, in vitro characterization, cholecystokinin receptor subtype 2 (CCK-2) binding in human tumor tissues, and cell internalization on CCK-2 receptor expressing AR42J cells, as well as biodistribution and small animal imaging in two different mouse xenograft models were studied.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">High receptor affinity and receptor-mediated uptake of the radioligands in AR42J cells was confirmed in vitro. (111)In-labeled cyclic DOTA-peptides showed a specific tumor uptake of ~1% ID/g in vivo, (68)Ga-labeled analogs of ~3% ID/g. Small animal SPECT imaging resulted to be superior with (111)In-DOTA-cyclo-MG2 in comparison with (111)In-DOTA-cyclo-MG1.</AbstractText><AbstractText Label="CONCLUSIONS" NlmCategory="CONCLUSIONS">Cyclic DOTA-minigastrin analogs are promising candidates for gastrin receptor scintigraphy and targeted radionuclide therapy.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>von Guggenberg</LastName><ForeName>Elisabeth</ForeName><Initials>E</Initials><Affiliation>Department of Nuclear Medicine, Innsbruck Medical University, Anichstrasse 35, 6020, Innsbruck, Austria. elisabeth.vonguggenberg@uki.at</Affiliation></Author><Author ValidYN="Y"><LastName>Rangger</LastName><ForeName>Christine</ForeName><Initials>C</Initials></Author><Author ValidYN="Y"><LastName>Sosabowski</LastName><ForeName>Jane</ForeName><Initials>J</Initials></Author><Author ValidYN="Y"><LastName>Laverman</LastName><ForeName>Peter</ForeName><Initials>P</Initials></Author><Author ValidYN="Y"><LastName>Reubi</LastName><ForeName>Jean-Claude</ForeName><Initials>JC</Initials></Author><Author ValidYN="Y"><LastName>Virgolini</LastName><ForeName>Irene Johanna</ForeName><Initials>IJ</Initials></Author><Author ValidYN="Y"><LastName>Decristoforo</LastName><ForeName>Clemens</ForeName><Initials>C</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>Mol Imaging Biol</MedlineTA><NlmUniqueID>101125610</NlmUniqueID><ISSNLinking>1536-1632</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Gallium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Gastrins</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>Receptors, Cholecystokinin</NameOfSubstance></Chemical><Chemical><RegistryNumber>60239-18-1</RegistryNumber><NameOfSubstance>1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid</NameOfSubstance></Chemical><Chemical><RegistryNumber>60748-07-4</RegistryNumber><NameOfSubstance>minigastrin</NameOfSubstance></Chemical></ChemicalList><SupplMeshList><SupplMeshName Type="Disease">Thyroid cancer, medullary</SupplMeshName></SupplMeshList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Evaluation, Preclinical</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Gallium Radioisotopes</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Gastrins</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Inbred BALB C</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, SCID</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Cholecystokinin</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Thyroid Neoplasms</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tomography, Emission-Computed, Single-Photon</DescriptorName><QualifierName MajorTopicYN="Y">methods</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="entrez"><Year>2011</Year><Month>7</Month><Day>7</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2011</Year><Month>7</Month><Day>7</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2012</Year><Month>10</Month><Day>30</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="doi">10.1007/s11307-011-0506-2</ArticleId><ArticleId IdType="pubmed">21732165</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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