Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors.
Identifieur interne : 003B71 ( Main/Exploration ); précédent : 003B70; suivant : 003B72Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors.
Auteurs : RBID : pubmed:10452322English descriptors
- KwdEn :
- Adult, Aged, Amino Acid Sequence, Animals, Carcinoma, Medullary (metabolism), Carcinoma, Medullary (radionuclide imaging), Carcinoma, Medullary (therapy), Carcinoma, Small Cell (metabolism), Carcinoma, Small Cell (radionuclide imaging), Carcinoma, Small Cell (therapy), Cholecystokinin (administration & dosage), Cholecystokinin (metabolism), Data Interpretation, Statistical, Female, Gastrins (administration & dosage), Gastrins (metabolism), Humans, Indium Radioisotopes (diagnostic use), Iodine Radioisotopes (diagnostic use), Isotope Labeling, Lung Neoplasms (metabolism), Lung Neoplasms (radionuclide imaging), Lung Neoplasms (therapy), Lymphatic Metastasis (radionuclide imaging), Male, Mice, Mice, Nude, Middle Aged, Molecular Sequence Data, Neoplasm Metastasis (radionuclide imaging), Neoplasms, Experimental (radionuclide imaging), Neoplasms, Experimental (therapy), Peptides (administration & dosage), Peptides (genetics), Radioisotopes (diagnostic use), Receptors, Cholecystokinin (analysis), Receptors, Cholecystokinin (metabolism), Thyroid Neoplasms (metabolism), Thyroid Neoplasms (radionuclide imaging), Thyroid Neoplasms (therapy).
- MESH :
- chemical , administration & dosage : Cholecystokinin, Gastrins, Peptides.
- chemical , analysis : Receptors, Cholecystokinin.
- chemical , diagnostic use : Indium Radioisotopes, Iodine Radioisotopes, Radioisotopes.
- chemical , genetics : Peptides.
- metabolism : Carcinoma, Medullary, Carcinoma, Small Cell, Cholecystokinin, Gastrins, Lung Neoplasms, Receptors, Cholecystokinin, Thyroid Neoplasms.
- radionuclide imaging : Carcinoma, Medullary, Carcinoma, Small Cell, Lung Neoplasms, Lymphatic Metastasis, Neoplasm Metastasis, Neoplasms, Experimental, Thyroid Neoplasms.
- therapy : Carcinoma, Medullary, Carcinoma, Small Cell, Lung Neoplasms, Neoplasms, Experimental, Thyroid Neoplasms.
- Adult, Aged, Amino Acid Sequence, Animals, Data Interpretation, Statistical, Female, Humans, Isotope Labeling, Male, Mice, Mice, Nude, Middle Aged, Molecular Sequence Data.
Abstract
The high sensitivity of pentagastrin stimulation in detecting primary or metastatic medullary thyroid cancer (MTC) suggests widespread expression of the corresponding receptor type on human MTC. Indeed, autoradiographic studies have demonstrated cholecystokinin (CCK)-B/gastrin receptors not only in more than 90% of MTCs but also in a high percentage of small cell lung cancers, some ovarian cancers, astrocytomas and potentially a variety of adenocarcinomas. The aim of this study was to systematically screen and optimize, in a preclinical model and a pilot clinical study, suitable radioligands for targeting CCK-B receptors in vivo.
PubMed: 10452322
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors.</title><author><name sortKey="Behr, T M" uniqKey="Behr T">T M Behr</name><affiliation wicri:level="3"><nlm:affiliation>Department of Nuclear Medicine, Georg-August-University, Göttingen, Germany.</nlm:affiliation><country xml:lang="fr">Allemagne</country><wicri:regionArea>Department of Nuclear Medicine, Georg-August-University, Göttingen</wicri:regionArea><placeName><region type="land" nuts="2">Basse-Saxe</region><settlement type="city">Göttingen</settlement></placeName></affiliation></author><author><name sortKey="Jenner, N" uniqKey="Jenner N">N Jenner</name></author><author><name sortKey="Behe, M" uniqKey="Behe M">M Béhé</name></author><author><name sortKey="Angerstein, C" uniqKey="Angerstein C">C Angerstein</name></author><author><name sortKey="Gratz, S" uniqKey="Gratz S">S Gratz</name></author><author><name sortKey="Raue, F" uniqKey="Raue F">F Raue</name></author><author><name sortKey="Becker, W" uniqKey="Becker W">W Becker</name></author></titleStmt><publicationStmt><date when="1999">1999</date><idno type="RBID">pubmed:10452322</idno><idno type="pmid">10452322</idno><idno type="wicri:Area/Main/Corpus">003E24</idno><idno type="wicri:Area/Main/Curation">003E24</idno><idno type="wicri:Area/Main/Exploration">003B71</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Adult</term><term>Aged</term><term>Amino Acid Sequence</term><term>Animals</term><term>Carcinoma, Medullary (metabolism)</term><term>Carcinoma, Medullary (radionuclide imaging)</term><term>Carcinoma, Medullary (therapy)</term><term>Carcinoma, Small Cell (metabolism)</term><term>Carcinoma, Small Cell (radionuclide imaging)</term><term>Carcinoma, Small Cell (therapy)</term><term>Cholecystokinin (administration & dosage)</term><term>Cholecystokinin (metabolism)</term><term>Data Interpretation, Statistical</term><term>Female</term><term>Gastrins (administration & dosage)</term><term>Gastrins (metabolism)</term><term>Humans</term><term>Indium Radioisotopes (diagnostic use)</term><term>Iodine Radioisotopes (diagnostic use)</term><term>Isotope Labeling</term><term>Lung Neoplasms (metabolism)</term><term>Lung Neoplasms (radionuclide imaging)</term><term>Lung Neoplasms (therapy)</term><term>Lymphatic Metastasis (radionuclide imaging)</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Middle Aged</term><term>Molecular Sequence Data</term><term>Neoplasm Metastasis (radionuclide imaging)</term><term>Neoplasms, Experimental (radionuclide imaging)</term><term>Neoplasms, Experimental (therapy)</term><term>Peptides (administration & dosage)</term><term>Peptides (genetics)</term><term>Radioisotopes (diagnostic use)</term><term>Receptors, Cholecystokinin (analysis)</term><term>Receptors, Cholecystokinin (metabolism)</term><term>Thyroid Neoplasms (metabolism)</term><term>Thyroid Neoplasms (radionuclide imaging)</term><term>Thyroid Neoplasms (therapy)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="administration & dosage" xml:lang="en"><term>Cholecystokinin</term><term>Gastrins</term><term>Peptides</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analysis" xml:lang="en"><term>Receptors, Cholecystokinin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Indium Radioisotopes</term><term>Iodine Radioisotopes</term><term>Radioisotopes</term></keywords><keywords scheme="MESH" type="chemical" qualifier="genetics" xml:lang="en"><term>Peptides</term></keywords><keywords scheme="MESH" qualifier="metabolism" xml:lang="en"><term>Carcinoma, Medullary</term><term>Carcinoma, Small Cell</term><term>Cholecystokinin</term><term>Gastrins</term><term>Lung Neoplasms</term><term>Receptors, Cholecystokinin</term><term>Thyroid Neoplasms</term></keywords><keywords scheme="MESH" qualifier="radionuclide imaging" xml:lang="en"><term>Carcinoma, Medullary</term><term>Carcinoma, Small Cell</term><term>Lung Neoplasms</term><term>Lymphatic Metastasis</term><term>Neoplasm Metastasis</term><term>Neoplasms, Experimental</term><term>Thyroid Neoplasms</term></keywords><keywords scheme="MESH" qualifier="therapy" xml:lang="en"><term>Carcinoma, Medullary</term><term>Carcinoma, Small Cell</term><term>Lung Neoplasms</term><term>Neoplasms, Experimental</term><term>Thyroid Neoplasms</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Adult</term><term>Aged</term><term>Amino Acid Sequence</term><term>Animals</term><term>Data Interpretation, Statistical</term><term>Female</term><term>Humans</term><term>Isotope Labeling</term><term>Male</term><term>Mice</term><term>Mice, Nude</term><term>Middle Aged</term><term>Molecular Sequence Data</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The high sensitivity of pentagastrin stimulation in detecting primary or metastatic medullary thyroid cancer (MTC) suggests widespread expression of the corresponding receptor type on human MTC. Indeed, autoradiographic studies have demonstrated cholecystokinin (CCK)-B/gastrin receptors not only in more than 90% of MTCs but also in a high percentage of small cell lung cancers, some ovarian cancers, astrocytomas and potentially a variety of adenocarcinomas. The aim of this study was to systematically screen and optimize, in a preclinical model and a pilot clinical study, suitable radioligands for targeting CCK-B receptors in vivo.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">10452322</PMID><DateCreated><Year>1999</Year><Month>09</Month><Day>02</Day></DateCreated><DateCompleted><Year>1999</Year><Month>09</Month><Day>02</Day></DateCompleted><DateRevised><Year>2006</Year><Month>11</Month><Day>15</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Print">0161-5505</ISSN><JournalIssue CitedMedium="Print"><Volume>40</Volume><Issue>6</Issue><PubDate><Year>1999</Year><Month>Jun</Month></PubDate></JournalIssue><Title>Journal of nuclear medicine : official publication, Society of Nuclear Medicine</Title><ISOAbbreviation>J. Nucl. Med.</ISOAbbreviation></Journal><ArticleTitle>Radiolabeled peptides for targeting cholecystokinin-B/gastrin receptor-expressing tumors.</ArticleTitle><Pagination><MedlinePgn>1029-44</MedlinePgn></Pagination><Abstract><AbstractText Label="UNLABELLED">The high sensitivity of pentagastrin stimulation in detecting primary or metastatic medullary thyroid cancer (MTC) suggests widespread expression of the corresponding receptor type on human MTC. Indeed, autoradiographic studies have demonstrated cholecystokinin (CCK)-B/gastrin receptors not only in more than 90% of MTCs but also in a high percentage of small cell lung cancers, some ovarian cancers, astrocytomas and potentially a variety of adenocarcinomas. The aim of this study was to systematically screen and optimize, in a preclinical model and a pilot clinical study, suitable radioligands for targeting CCK-B receptors in vivo.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">A variety of CCK/gastrin-related peptides, all bearing the C-terminal CCK receptor-binding tetrapeptide sequence Trp-Met-Asp-PheNH2 or derivatives thereof, were studied. They were radioiodinated by the lodogen or Bolton-Hunter procedures. The peptides were members of the gastrin or CCK families, which differ by the intramolecular position of a tyrosyl moiety. Their stability and affinity were studied in vitro and in vivo; their biodistribution and therapeutic efficacy were tested in nude mice bearing subcutaneous human MTC xenografts. Diethylenetriamine pentaacetic acid (DTPA) derivatives of suitable peptides were synthesized successfully, and their preclinical and initial clinical evaluations were performed, labeled with 111In.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">All members of the CCK or gastrin families were stable in serum (with half-lives of several hours at 37 degrees C); nevertheless, the stability of those peptides bearing N-terminal pGlu residues or D-amino acids was significantly higher. In accordance with their comparably low affinity, nonsulfated members of the CCK family showed fairly low uptake in the tumor and other CCK-B receptor-expressing tissues. Sulfated CCK derivatives performed significantly better but also displayed a comparably high uptake in normal CCK-A receptor-expressing tissues. This effect was probably due to their similar affinity for both CCK-A and CCK-B receptors. Best tumor uptake and tumor-to-nontumor ratios were obtained with members of the gastrin family because of their selectivity and affinity for the CCK-B receptor subtype. Pilot therapy experiments in MTC-bearing animals showed significant antitumor efficacy compared with untreated controls. DTPA derivatives of minigastrin were successfully developed. In a pilot clinical study, radioiodinated and 111In-labeled derivatives showed excellent targeting of physiological CCK-B receptor-expressing organs, as well as all known tumor sites.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">CCK/gastrin analogs may be a useful new class of receptor-binding peptides for diagnosis and therapy of CCK-B receptor-expressing tumors, such as MTC or small cell lung cancer. Nonsulfated gastrin derivatives may be preferable because of their CCK-B receptor selectivity, hence lower accretion in normal CCK-A receptor-expressing organs.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Behr</LastName><ForeName>T M</ForeName><Initials>TM</Initials><Affiliation>Department of Nuclear Medicine, Georg-August-University, Göttingen, Germany.</Affiliation></Author><Author ValidYN="Y"><LastName>Jenner</LastName><ForeName>N</ForeName><Initials>N</Initials></Author><Author ValidYN="Y"><LastName>Béhé</LastName><ForeName>M</ForeName><Initials>M</Initials></Author><Author ValidYN="Y"><LastName>Angerstein</LastName><ForeName>C</ForeName><Initials>C</Initials></Author><Author ValidYN="Y"><LastName>Gratz</LastName><ForeName>S</ForeName><Initials>S</Initials></Author><Author ValidYN="Y"><LastName>Raue</LastName><ForeName>F</ForeName><Initials>F</Initials></Author><Author ValidYN="Y"><LastName>Becker</LastName><ForeName>W</ForeName><Initials>W</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Comparative Study</PublicationType><PublicationType>Journal Article</PublicationType><PublicationType>Research Support, Non-U.S. Gov't</PublicationType></PublicationTypeList></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>Gastrins</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Iodine Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Peptides</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Cholecystokinin</NameOfSubstance></Chemical><Chemical><RegistryNumber>9011-97-6</RegistryNumber><NameOfSubstance>Cholecystokinin</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Adult</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Aged</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Amino Acid Sequence</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Carcinoma, Medullary</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName><QualifierName MajorTopicYN="N">therapy</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Carcinoma, Small Cell</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName><QualifierName MajorTopicYN="N">therapy</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Cholecystokinin</DescriptorName><QualifierName MajorTopicYN="N">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Data Interpretation, Statistical</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Gastrins</DescriptorName><QualifierName MajorTopicYN="N">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Iodine Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Isotope Labeling</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lung Neoplasms</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName><QualifierName MajorTopicYN="N">therapy</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Lymphatic Metastasis</DescriptorName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Middle Aged</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Molecular Sequence Data</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasm Metastasis</DescriptorName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Neoplasms, Experimental</DescriptorName><QualifierName MajorTopicYN="N">radionuclide imaging</QualifierName><QualifierName MajorTopicYN="N">therapy</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Peptides</DescriptorName><QualifierName MajorTopicYN="N">administration & dosage</QualifierName><QualifierName MajorTopicYN="N">genetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radioisotopes</DescriptorName><QualifierName MajorTopicYN="Y">diagnostic use</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Receptors, Cholecystokinin</DescriptorName><QualifierName MajorTopicYN="N">analysis</QualifierName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Thyroid Neoplasms</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName><QualifierName MajorTopicYN="Y">radionuclide imaging</QualifierName><QualifierName MajorTopicYN="N">therapy</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate PubStatus="pubmed"><Year>1999</Year><Month>8</Month><Day>19</Day></PubMedPubDate><PubMedPubDate PubStatus="medline"><Year>1999</Year><Month>8</Month><Day>19</Day><Hour>0</Hour><Minute>1</Minute></PubMedPubDate><PubMedPubDate PubStatus="entrez"><Year>1999</Year><Month>8</Month><Day>19</Day><Hour>0</Hour><Minute>0</Minute></PubMedPubDate></History><PublicationStatus>ppublish</PublicationStatus><ArticleIdList><ArticleId IdType="pubmed">10452322</ArticleId></ArticleIdList></PubmedData></pubmed></record>Pour manipuler ce document sous Unix (Dilib)
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