Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.
Identifieur interne : 000305 ( Main/Exploration ); précédent : 000304; suivant : 000306Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.
Auteurs : RBID : pubmed:24094035English descriptors
- KwdEn :
- Animals, Cell Line, Tumor, Heterocyclic Compounds, 1-Ring (chemical synthesis), Heterocyclic Compounds, 1-Ring (diagnostic use), Heterocyclic Compounds, 1-Ring (metabolism), Heterocyclic Compounds, 1-Ring (pharmacokinetics), Humans, Indium Radioisotopes (diagnostic use), Mice, Mice, SCID, Molecular Structure, Neoplasms, Experimental (diagnosis), Receptors, Bombesin (chemistry), Receptors, Bombesin (metabolism), Tissue Distribution.
- MESH :
- chemical , chemical synthesis : Heterocyclic Compounds, 1-Ring.
- chemical , chemistry : Receptors, Bombesin.
- chemical , diagnostic use : Heterocyclic Compounds, 1-Ring, Indium Radioisotopes.
- chemical , metabolism : Heterocyclic Compounds, 1-Ring, Receptors, Bombesin.
- chemical , pharmacokinetics : Heterocyclic Compounds, 1-Ring.
- diagnosis : Neoplasms, Experimental.
- Animals, Cell Line, Tumor, Humans, Mice, Mice, SCID, Molecular Structure, Tissue Distribution.
Abstract
Radiolabeled analogs of the frog tetradecapeptide bombesin (BBN) have been proposed for diagnosis and therapy of gastrin releasing peptide receptor (GRPR)-expressing tumors. Following a different and yet unexplored approach, we have developed four novel (111)In-labeled truncated analogs of the human 27-mer GRP after conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) at the N-terminus of GRP(13/14/17/18-27) fragments. Analog affinities for the human GRPR determined against [(125)I-Tyr(4)]BBN were at the nanomolar level and dependent on truncation site. The respective (111)In radioligands specifically internalized in GRPR-expressing PC-3 cells. The shorter chain [(111)In-DOTA]GRP(17/18-27) analogs showed higher metabolic stability in mice. Radioligands specifically localized in human PC-3 xenografts in SCID mice, with [(111)In-DOTA]GRP(17-27) exhibiting the most favorable pharmacokinetic profile. This study has demonstrated the efficacy of human GRP-based radiopeptides to target GRPR-positive lesions in vivo and has revealed the impact of GRP chain length on key biological parameters of resulting radiotracers.
DOI: 10.1021/jm4010237
PubMed: 24094035
Links toward previous steps (curation, corpus...)
Le document en format XML
<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.</title><author><name sortKey="Marsouvanidis, Panteleimon J" uniqKey="Marsouvanidis P">Panteleimon J Marsouvanidis</name><affiliation wicri:level="1"><nlm:affiliation>Molecular Radiopharmacy, INRASTES, National Center for Scientific Research "Demokritos" , GR-153 10 Athens, Greece.</nlm:affiliation><country xml:lang="fr">Grèce</country><wicri:regionArea>Molecular Radiopharmacy, INRASTES, National Center for Scientific Research "Demokritos" , GR-153 10 Athens</wicri:regionArea></affiliation></author><author><name sortKey="Maina, Theodosia" uniqKey="Maina T">Theodosia Maina</name></author><author><name sortKey="Sallegger, Werner" uniqKey="Sallegger W">Werner Sallegger</name></author><author><name sortKey="Krenning, Eric P" uniqKey="Krenning E">Eric P Krenning</name></author><author><name sortKey="De Jong, Marion" uniqKey="De Jong M">Marion de Jong</name></author><author><name sortKey="Nock, Berthold A" uniqKey="Nock B">Berthold A Nock</name></author></titleStmt><publicationStmt><date when="2013">2013</date><idno type="doi">10.1021/jm4010237</idno><idno type="RBID">pubmed:24094035</idno><idno type="pmid">24094035</idno><idno type="wicri:Area/Main/Corpus">000382</idno><idno type="wicri:Area/Main/Curation">000382</idno><idno type="wicri:Area/Main/Exploration">000305</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Heterocyclic Compounds, 1-Ring (chemical synthesis)</term><term>Heterocyclic Compounds, 1-Ring (diagnostic use)</term><term>Heterocyclic Compounds, 1-Ring (metabolism)</term><term>Heterocyclic Compounds, 1-Ring (pharmacokinetics)</term><term>Humans</term><term>Indium Radioisotopes (diagnostic use)</term><term>Mice</term><term>Mice, SCID</term><term>Molecular Structure</term><term>Neoplasms, Experimental (diagnosis)</term><term>Receptors, Bombesin (chemistry)</term><term>Receptors, Bombesin (metabolism)</term><term>Tissue Distribution</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemical synthesis" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term></keywords><keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Receptors, Bombesin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Indium Radioisotopes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term><term>Receptors, Bombesin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Heterocyclic Compounds, 1-Ring</term></keywords><keywords scheme="MESH" qualifier="diagnosis" xml:lang="en"><term>Neoplasms, Experimental</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Cell Line, Tumor</term><term>Humans</term><term>Mice</term><term>Mice, SCID</term><term>Molecular Structure</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Radiolabeled analogs of the frog tetradecapeptide bombesin (BBN) have been proposed for diagnosis and therapy of gastrin releasing peptide receptor (GRPR)-expressing tumors. Following a different and yet unexplored approach, we have developed four novel (111)In-labeled truncated analogs of the human 27-mer GRP after conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) at the N-terminus of GRP(13/14/17/18-27) fragments. Analog affinities for the human GRPR determined against [(125)I-Tyr(4)]BBN were at the nanomolar level and dependent on truncation site. The respective (111)In radioligands specifically internalized in GRPR-expressing PC-3 cells. The shorter chain [(111)In-DOTA]GRP(17/18-27) analogs showed higher metabolic stability in mice. Radioligands specifically localized in human PC-3 xenografts in SCID mice, with [(111)In-DOTA]GRP(17-27) exhibiting the most favorable pharmacokinetic profile. This study has demonstrated the efficacy of human GRP-based radiopeptides to target GRPR-positive lesions in vivo and has revealed the impact of GRP chain length on key biological parameters of resulting radiotracers.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">24094035</PMID><DateCreated><Year>2014</Year><Month>01</Month><Day>03</Day></DateCreated><DateCompleted><Year>2014</Year><Month>03</Month><Day>18</Day></DateCompleted><Article PubModel="Print-Electronic"><Journal><ISSN IssnType="Electronic">1520-4804</ISSN><JournalIssue CitedMedium="Internet"><Volume>56</Volume><Issue>21</Issue><PubDate><Year>2013</Year><Month>Nov</Month><Day>14</Day></PubDate></JournalIssue><Title>Journal of medicinal chemistry</Title><ISOAbbreviation>J. Med. Chem.</ISOAbbreviation></Journal><ArticleTitle>Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.</ArticleTitle><Pagination><MedlinePgn>8579-87</MedlinePgn></Pagination><ELocationID EIdType="doi" ValidYN="Y">10.1021/jm4010237</ELocationID><Abstract><AbstractText>Radiolabeled analogs of the frog tetradecapeptide bombesin (BBN) have been proposed for diagnosis and therapy of gastrin releasing peptide receptor (GRPR)-expressing tumors. Following a different and yet unexplored approach, we have developed four novel (111)In-labeled truncated analogs of the human 27-mer GRP after conjugation of 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) at the N-terminus of GRP(13/14/17/18-27) fragments. Analog affinities for the human GRPR determined against [(125)I-Tyr(4)]BBN were at the nanomolar level and dependent on truncation site. The respective (111)In radioligands specifically internalized in GRPR-expressing PC-3 cells. The shorter chain [(111)In-DOTA]GRP(17/18-27) analogs showed higher metabolic stability in mice. Radioligands specifically localized in human PC-3 xenografts in SCID mice, with [(111)In-DOTA]GRP(17-27) exhibiting the most favorable pharmacokinetic profile. This study has demonstrated the efficacy of human GRP-based radiopeptides to target GRPR-positive lesions in vivo and has revealed the impact of GRP chain length on key biological parameters of resulting radiotracers.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Marsouvanidis</LastName><ForeName>Panteleimon J</ForeName><Initials>PJ</Initials><Affiliation>Molecular Radiopharmacy, INRASTES, National Center for Scientific Research "Demokritos" , GR-153 10 Athens, Greece.</Affiliation></Author><Author ValidYN="Y"><LastName>Maina</LastName><ForeName>Theodosia</ForeName><Initials>T</Initials></Author><Author ValidYN="Y"><LastName>Sallegger</LastName><ForeName>Werner</ForeName><Initials>W</Initials></Author><Author ValidYN="Y"><LastName>Krenning</LastName><ForeName>Eric P</ForeName><Initials>EP</Initials></Author><Author ValidYN="Y"><LastName>de Jong</LastName><ForeName>Marion</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Nock</LastName><ForeName>Berthold A</ForeName><Initials>BA</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Comparative Study</PublicationType><PublicationType>Journal Article</PublicationType></PublicationTypeList><ArticleDate DateType="Electronic"><Year>2013</Year><Month>10</Month><Day>23</Day></ArticleDate></Article><MedlineJournalInfo><Country>United States</Country><MedlineTA>J Med Chem</MedlineTA><NlmUniqueID>9716531</NlmUniqueID><ISSNLinking>0022-2623</ISSNLinking></MedlineJournalInfo><ChemicalList><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, Bombesin</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">Cell Line, Tumor</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Heterocyclic Compounds, 1-Ring</DescriptorName><QualifierName MajorTopicYN="N">chemical synthesis</QualifierName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, SCID</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Molecular Structure</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasms, Experimental</DescriptorName><QualifierName MajorTopicYN="Y">diagnosis</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Bombesin</DescriptorName><QualifierName MajorTopicYN="Y">chemistry</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="aheadofprint"><Year>2013</Year><Month>10</Month><Day>23</Day></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>2013</Year><Month>10</Month><Day>8</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="pubmed"><Year>2013</Year><Month>10</Month><Day>8</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>2014</Year><Month>3</Month><Day>19</Day><Hour>6</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="doi">10.1021/jm4010237</ArticleId><ArticleId IdType="pubmed">24094035</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
EXPLOR_STEP=IndiumV2/Data/Main/Exploration
HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000305 | SxmlIndent | more
Ou
HfdSelect -h $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd -nk 000305 | SxmlIndent | more
Pour mettre un lien sur cette page dans le réseau Wicri
{{Explor lien
|wiki= *** parameter Area/wikiCode missing ***
|area= IndiumV2
|flux= Main
|étape= Exploration
|type= RBID
|clé= pubmed:24094035
|texte= Tumor diagnosis with new 111In-radioligands based on truncated human gastrin releasing peptide sequences: synthesis and preclinical comparison.
}}
Pour générer des pages wiki
HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i -Sk "pubmed:24094035" \
| HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd \
| NlmPubMed2Wicri -a IndiumV2
| This area was generated with Dilib version V0.5.76. |  |