Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.
Identifieur interne : 001717 ( Main/Exploration ); précédent : 001716; suivant : 001718Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.
Auteurs : RBID : pubmed:20396884English descriptors
- KwdEn :
- Cell Line, Chelating Agents (chemistry), Heterocyclic Compounds, 1-Ring (chemistry), Humans, Protein Transport (drug effects), Receptors, Somatostatin (agonists), Receptors, Somatostatin (antagonists & inhibitors), Receptors, Somatostatin (metabolism), Somatostatin (analogs & derivatives), Somatostatin (chemistry), Somatostatin (metabolism), Somatostatin (pharmacology).
- MESH :
- chemical , agonists : Receptors, Somatostatin.
- chemical , analogs & derivatives : Somatostatin.
- chemical , antagonists & inhibitors : Receptors, Somatostatin.
- chemical , chemistry : Chelating Agents, Heterocyclic Compounds, 1-Ring, Somatostatin.
- drug effects : Protein Transport.
- chemical , metabolism : Receptors, Somatostatin, Somatostatin.
- chemical , pharmacology : Somatostatin.
- Cell Line, Humans.
Abstract
Peptide receptor targeting has become an increasingly attractive method to target tumors diagnostically and radiotherapeutically. Peptides linked to a variety of chelators have been developed for this purpose. They have, however, rarely been tested for their agonistic or antagonistic properties. We report here on a somatostatin antagonist that switched to an agonist upon coupling to a DOTA chelator.
DOI: 10.1007/s00259-010-1445-x
PubMed: 20396884
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.</title><author><name sortKey="Reubi, Jean Claude" uniqKey="Reubi J">Jean Claude Reubi</name><affiliation wicri:level="1"><nlm:affiliation>Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, 3010 Berne, Switzerland. reubi@pathology.unibe.ch</nlm:affiliation><country xml:lang="fr">Suisse</country><wicri:regionArea>Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, 3010 Berne</wicri:regionArea></affiliation></author><author><name sortKey="Erchegyi, Judit" uniqKey="Erchegyi J">Judit Erchegyi</name></author><author><name sortKey="Cescato, Renzo" uniqKey="Cescato R">Renzo Cescato</name></author><author><name sortKey="Waser, Beatrice" uniqKey="Waser B">Beatrice Waser</name></author><author><name sortKey="Rivier, Jean E" uniqKey="Rivier J">Jean E Rivier</name></author></titleStmt><publicationStmt><date when="2010">2010</date><idno type="doi">10.1007/s00259-010-1445-x</idno><idno type="RBID">pubmed:20396884</idno><idno type="pmid">20396884</idno><idno type="wicri:Area/Main/Corpus">001964</idno><idno type="wicri:Area/Main/Curation">001964</idno><idno type="wicri:Area/Main/Exploration">001717</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Cell Line</term><term>Chelating Agents (chemistry)</term><term>Heterocyclic Compounds, 1-Ring (chemistry)</term><term>Humans</term><term>Protein Transport (drug effects)</term><term>Receptors, Somatostatin (agonists)</term><term>Receptors, Somatostatin (antagonists & inhibitors)</term><term>Receptors, Somatostatin (metabolism)</term><term>Somatostatin (analogs & derivatives)</term><term>Somatostatin (chemistry)</term><term>Somatostatin (metabolism)</term><term>Somatostatin (pharmacology)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="agonists" xml:lang="en"><term>Receptors, Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="antagonists & inhibitors" xml:lang="en"><term>Receptors, Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Chelating Agents</term><term>Heterocyclic Compounds, 1-Ring</term><term>Somatostatin</term></keywords><keywords scheme="MESH" qualifier="drug effects" xml:lang="en"><term>Protein Transport</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Receptors, Somatostatin</term><term>Somatostatin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Somatostatin</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Cell Line</term><term>Humans</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Peptide receptor targeting has become an increasingly attractive method to target tumors diagnostically and radiotherapeutically. Peptides linked to a variety of chelators have been developed for this purpose. They have, however, rarely been tested for their agonistic or antagonistic properties. We report here on a somatostatin antagonist that switched to an agonist upon coupling to a DOTA chelator.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">20396884</PMID><DateCreated><Year>2010</Year><Month>08</Month><Day>04</Day></DateCreated><DateCompleted><Year>2011</Year><Month>01</Month><Day>04</Day></DateCompleted><DateRevised><Year>2013</Year><Month>10</Month><Day>23</Day></DateRevised><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1619-7089</ISSN><JournalIssue CitedMedium="Internet"><Volume>37</Volume><Issue>8</Issue><PubDate><Year>2010</Year><Month>Aug</Month></PubDate></JournalIssue><Title>European journal of nuclear medicine and molecular imaging</Title><ISOAbbreviation>Eur. J. Nucl. Med. Mol. Imaging</ISOAbbreviation></Journal><ArticleTitle>Switch from antagonist to agonist after addition of a DOTA chelator to a somatostatin analog.</ArticleTitle><Pagination><MedlinePgn>1551-8</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1007/s00259-010-1445-x</ELocationID><Abstract><AbstractText Label="PURPOSE" NlmCategory="OBJECTIVE">Peptide receptor targeting has become an increasingly attractive method to target tumors diagnostically and radiotherapeutically. Peptides linked to a variety of chelators have been developed for this purpose. They have, however, rarely been tested for their agonistic or antagonistic properties. We report here on a somatostatin antagonist that switched to an agonist upon coupling to a DOTA chelator.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">Two novel somatostatin analogs, 406-040-15 and its DOTA-coupled counterpart 406-051-20, with and without cold Indium labeling, were tested for their somatostatin receptor subtypes 1-5 (sst(1)-sst(5)) binding affinity using receptor autoradiography. Moreover, they were tested functionally for their ability to affect sst(2) and sst(3) internalization in vitro in HEK293 cells stably expressing the human sst(2) or sst(3) receptor, using an immunofluorescence microscopy-based internalization assay.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">All three compounds were characterized as pan-somatostatin analogs having a high affinity for all five sst. In the sst(2) internalization assay, all three compounds showed an identical behavior, namely, a weak agonistic effect complemented by a weak antagonistic effect, compatible with the behavior of a partial agonist. Conversely, in the sst(3) internalization assay, 406-040-15 was a full antagonist whereas its DOTA-coupled counterpart, 406-051-20, with and without Indium labeling, switched to a full agonist.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Adding the DOTA chelator to the somatostatin analog 406-040-15 triggers a switch at sst(3) receptor from an antagonist to an agonist. This indicates that potential radioligands for tumor targeting should always be tested functionally before further development, in particular if a chelator is added.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Reubi</LastName><ForeName>Jean Claude</ForeName><Initials>JC</Initials><Affiliation>Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, PO Box 62, Murtenstrasse 31, 3010 Berne, Switzerland. reubi@pathology.unibe.ch</Affiliation></Author><Author ValidYN="Y"><LastName>Erchegyi</LastName><ForeName>Judit</ForeName><Initials>J</Initials></Author><Author ValidYN="Y"><LastName>Cescato</LastName><ForeName>Renzo</ForeName><Initials>R</Initials></Author><Author ValidYN="Y"><LastName>Waser</LastName><ForeName>Beatrice</ForeName><Initials>B</Initials></Author><Author ValidYN="Y"><LastName>Rivier</LastName><ForeName>Jean E</ForeName><Initials>JE</Initials></Author></AuthorList><Language>eng</Language><GrantList CompleteYN="Y"><Grant><GrantID>DK059953</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>R01 DK059953-01A1</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>R01 DK059953-02</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>R01 DK059953-03</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>R01 DK059953-04</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant><Grant><GrantID>R01 DK059953-05</GrantID><Acronym>DK</Acronym><Agency>NIDDK NIH HHS</Agency><Country>United States</Country></Grant></GrantList><PublicationTypeList><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, N.I.H., Extramural</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2010</Year><Month>04</Month><Day>16</Day></ArticleDate></Article><MedlineJournalInfo><Country>Germany</Country><MedlineTA>Eur J Nucl Med Mol Imaging</MedlineTA><NlmUniqueID>101140988</NlmUniqueID><ISSNLinking>1619-7070</ISSNLinking></MedlineJournalInfo><ChemicalList><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Chelating Agents</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Heterocyclic Compounds, 1-Ring</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Somatostatin</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>somatostatin receptor sst2A</NameOfSubstance></Chemical><Chemical><RegistryNumber>51110-01-1</RegistryNumber><NameOfSubstance>Somatostatin</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><CommentsCorrectionsList><CommentsCorrections RefType="Cites"><RefSource>Bioconjug Chem. 2008 Jan;19(1):192-200</RefSource><PMID Version="1">18020401</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>Eur J Nucl Med Mol Imaging. 2007 Aug;34(8):1198-208</RefSource><PMID Version="1">17262215</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>Clin Cancer Res. 2008 Apr 1;14(7):2019-27</RefSource><PMID Version="1">18381940</PMID></CommentsCorrections><CommentsCorrections RefType="Cites"><RefSource>J Med Chem. 2008 Jul 10;51(13):4030-7</RefSource><PMID 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MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Protein Transport</DescriptorName><QualifierName MajorTopicYN="N">drug effects</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Somatostatin</DescriptorName><QualifierName MajorTopicYN="Y">agonists</QualifierName><QualifierName MajorTopicYN="Y">antagonists & inhibitors</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Somatostatin</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">chemistry</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">pharmacology</QualifierName></MeshHeading></MeshHeadingList><OtherID Source="NLM">NIHMS257668</OtherID><OtherID Source="NLM">PMC3025705</OtherID></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="received"><Year>2009</Year><Month>12</Month><Day>10</Day></PubMedPubDate><PubMedPubDate PubStatus="accepted"><Year>2010</Year><Month>3</Month><Day>8</Day></PubMedPubDate><PubMedPubDate PubStatus="aheadofprint"><Year>2010</Year><Month>4</Month><Day>16</Day></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2010</Year><Month>4</Month><Day>17</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2010</Year><Month>4</Month><Day>17</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2011</Year><Month>1</Month><Day>5</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="doi">10.1007/s00259-010-1445-x</ArticleId><ArticleId IdType="pubmed">20396884</ArticleId><ArticleId IdType="pmc">PMC3025705</ArticleId><ArticleId IdType="mid">NIHMS257668</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour 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