Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs.
Identifieur interne : 002C09 ( Main/Exploration ); précédent : 002C08; suivant : 002C10Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs.
Auteurs : RBID : pubmed:15872357English descriptors
- KwdEn :
- Animals, Bombesin (analogs & derivatives), Bombesin (diagnostic use), Bombesin (pharmacokinetics), Disease Models, Animal, Drug Delivery Systems (methods), Female, Humans, Indium Radioisotopes (diagnostic use), Indium Radioisotopes (pharmacokinetics), Isotope Labeling (methods), Male, Metabolic Clearance Rate, Mice, Mice, Nude, Radiopharmaceuticals (diagnostic use), Radiopharmaceuticals (pharmacokinetics), Rats, Rats, Inbred Lew, Receptors, Bombesin (metabolism), Reproducibility of Results, Sensitivity and Specificity, Species Specificity, Technetium (diagnostic use), Technetium (pharmacokinetics), Tissue Distribution, Tumor Markers, Biological (metabolism).
- MESH :
- chemical , analogs & derivatives : Bombesin.
- chemical , diagnostic use : Bombesin, Indium Radioisotopes, Radiopharmaceuticals, Technetium.
- chemical , metabolism : Receptors, Bombesin, Tumor Markers, Biological.
- chemical , pharmacokinetics : Bombesin, Indium Radioisotopes, Radiopharmaceuticals, Technetium.
- methods : Drug Delivery Systems, Isotope Labeling.
- Animals, Disease Models, Animal, Female, Humans, Male, Metabolic Clearance Rate, Mice, Mice, Nude, Rats, Rats, Inbred Lew, Reproducibility of Results, Sensitivity and Specificity, Species Specificity, Tissue Distribution.
Abstract
The biologic profiles of [(99m)Tc]Demobesin 1 ([(99m)Tc-N(4)(0-1),bzlg(0),d-Phe(6),Leu-NHEt(13),des-Met(14)]BB(6-14)) and [(111)In]Z-070 were compared using various gastrin-releasing peptide receptor GRP-R)-expressing tissues of human and animal origin.
PubMed: 15872357
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<record><TEI><teiHeader><fileDesc><titleStmt><title xml:lang="en">Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs.</title><author><name sortKey="Maina, Theodosia" uniqKey="Maina T">Theodosia Maina</name><affiliation wicri:level="1"><nlm:affiliation>Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, 152 10 Ag. Paraskevi Arrikis, Athens, Greece. mainathe@rrp.demokritos.gr</nlm:affiliation><country xml:lang="fr">Grèce</country><wicri:regionArea>Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, 152 10 Ag. Paraskevi Arrikis, Athens</wicri:regionArea></affiliation></author><author><name sortKey="Nock, Berthold A" uniqKey="Nock B">Berthold A Nock</name></author><author><name sortKey="Zhang, Hanwen" uniqKey="Zhang H">Hanwen Zhang</name></author><author><name sortKey="Nikolopoulou, Anastasia" uniqKey="Nikolopoulou A">Anastasia Nikolopoulou</name></author><author><name sortKey="Waser, Beatrice" uniqKey="Waser B">Beatrice Waser</name></author><author><name sortKey="Reubi, Jean Claude" uniqKey="Reubi J">Jean-Claude Reubi</name></author><author><name sortKey="Maecke, Helmut R" uniqKey="Maecke H">Helmut R Maecke</name></author></titleStmt><publicationStmt><date when="2005">2005</date><idno type="RBID">pubmed:15872357</idno><idno type="pmid">15872357</idno><idno type="wicri:Area/Main/Corpus">002F08</idno><idno type="wicri:Area/Main/Curation">002F08</idno><idno type="wicri:Area/Main/Exploration">002C09</idno></publicationStmt></fileDesc><profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Animals</term><term>Bombesin (analogs & derivatives)</term><term>Bombesin (diagnostic use)</term><term>Bombesin (pharmacokinetics)</term><term>Disease Models, Animal</term><term>Drug Delivery Systems (methods)</term><term>Female</term><term>Humans</term><term>Indium Radioisotopes (diagnostic use)</term><term>Indium Radioisotopes (pharmacokinetics)</term><term>Isotope Labeling (methods)</term><term>Male</term><term>Metabolic Clearance Rate</term><term>Mice</term><term>Mice, Nude</term><term>Radiopharmaceuticals (diagnostic use)</term><term>Radiopharmaceuticals (pharmacokinetics)</term><term>Rats</term><term>Rats, Inbred Lew</term><term>Receptors, Bombesin (metabolism)</term><term>Reproducibility of Results</term><term>Sensitivity and Specificity</term><term>Species Specificity</term><term>Technetium (diagnostic use)</term><term>Technetium (pharmacokinetics)</term><term>Tissue Distribution</term><term>Tumor Markers, Biological (metabolism)</term></keywords><keywords scheme="MESH" type="chemical" qualifier="analogs & derivatives" xml:lang="en"><term>Bombesin</term></keywords><keywords scheme="MESH" type="chemical" qualifier="diagnostic use" xml:lang="en"><term>Bombesin</term><term>Indium Radioisotopes</term><term>Radiopharmaceuticals</term><term>Technetium</term></keywords><keywords scheme="MESH" type="chemical" qualifier="metabolism" xml:lang="en"><term>Receptors, Bombesin</term><term>Tumor Markers, Biological</term></keywords><keywords scheme="MESH" type="chemical" qualifier="pharmacokinetics" xml:lang="en"><term>Bombesin</term><term>Indium Radioisotopes</term><term>Radiopharmaceuticals</term><term>Technetium</term></keywords><keywords scheme="MESH" qualifier="methods" xml:lang="en"><term>Drug Delivery Systems</term><term>Isotope Labeling</term></keywords><keywords scheme="MESH" xml:lang="en"><term>Animals</term><term>Disease Models, Animal</term><term>Female</term><term>Humans</term><term>Male</term><term>Metabolic Clearance Rate</term><term>Mice</term><term>Mice, Nude</term><term>Rats</term><term>Rats, Inbred Lew</term><term>Reproducibility of Results</term><term>Sensitivity and Specificity</term><term>Species Specificity</term><term>Tissue Distribution</term></keywords></textClass></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">The biologic profiles of [(99m)Tc]Demobesin 1 ([(99m)Tc-N(4)(0-1),bzlg(0),d-Phe(6),Leu-NHEt(13),des-Met(14)]BB(6-14)) and [(111)In]Z-070 were compared using various gastrin-releasing peptide receptor GRP-R)-expressing tissues of human and animal origin.</div></front></TEI><pubmed><MedlineCitation Owner="NLM" Status="MEDLINE"><PMID Version="1">15872357</PMID><DateCreated><Year>2005</Year><Month>05</Month><Day>05</Day></DateCreated><DateCompleted><Year>2005</Year><Month>06</Month><Day>24</Day></DateCompleted><DateRevised><Year>2013</Year><Month>11</Month><Day>21</Day></DateRevised><Article PubModel="Print"><Journal><ISSN IssnType="Print">0161-5505</ISSN><JournalIssue CitedMedium="Print"><Volume>46</Volume><Issue>5</Issue><PubDate><Year>2005</Year><Month>May</Month></PubDate></JournalIssue><Title>Journal of nuclear medicine : official publication, Society of Nuclear Medicine</Title><ISOAbbreviation>J. Nucl. Med.</ISOAbbreviation></Journal><ArticleTitle>Species differences of bombesin analog interactions with GRP-R define the choice of animal models in the development of GRP-R-targeting drugs.</ArticleTitle><Pagination><MedlinePgn>823-30</MedlinePgn></Pagination><Abstract><AbstractText Label="UNLABELLED">The biologic profiles of [(99m)Tc]Demobesin 1 ([(99m)Tc-N(4)(0-1),bzlg(0),d-Phe(6),Leu-NHEt(13),des-Met(14)]BB(6-14)) and [(111)In]Z-070 were compared using various gastrin-releasing peptide receptor GRP-R)-expressing tissues of human and animal origin.</AbstractText><AbstractText Label="METHODS" NlmCategory="METHODS">The binding affinities of Demobesin 1, Z-070, and its metallated analogs were determined by receptor autoradiography on human cancer biopsy and mouse pancreas samples and by binding assays in rat AR4-2J and human PC-3 cell membranes. Biodistribution of [(99m)Tc]Demobesin 1 and [(111)In]Z-070 was compared in nude mice bearing AR4-2J and PC-3 xenografts.</AbstractText><AbstractText Label="RESULTS" NlmCategory="RESULTS">Demobesin 1, Z-070, and metallated Z-070 showed high affinity for the rat GRP-R in AR4-2J cell membranes (50% inhibitory concentration values = 0.17-0.45 nmol/L). In human PC-3 cell membranes, Demobesin 1 showed 11- to 15-fold higher affinity than the Z-070 peptides. These data were corroborated by results from human cancers and mouse pancreas. In AR4-2J and PC-3 tumor-bearing mice, [(99m)Tc]Demobesin 1 and [(111)In]Z-070 displayed similar uptake in the rat tumor. However, in the human PC-3 xenografts, [(99m)Tc]Demobesin 1 showed a 2- to 3-fold higher uptake than [(111)In]Z-070.</AbstractText><AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Considerable differences between rat or mouse and human GRP-R-expressing tissues were found for the in vitro and in vivo characteristics of 2 radiolabeled bombesin analogs. This finding may have a significant impact in the selection of experimental tools in the development of bombesin analogs for GRP-R-targeting applications in humans.</AbstractText></Abstract><AuthorList CompleteYN="Y"><Author ValidYN="Y"><LastName>Maina</LastName><ForeName>Theodosia</ForeName><Initials>T</Initials><Affiliation>Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, 152 10 Ag. Paraskevi Arrikis, Athens, Greece. mainathe@rrp.demokritos.gr</Affiliation></Author><Author ValidYN="Y"><LastName>Nock</LastName><ForeName>Berthold A</ForeName><Initials>BA</Initials></Author><Author ValidYN="Y"><LastName>Zhang</LastName><ForeName>Hanwen</ForeName><Initials>H</Initials></Author><Author ValidYN="Y"><LastName>Nikolopoulou</LastName><ForeName>Anastasia</ForeName><Initials>A</Initials></Author><Author ValidYN="Y"><LastName>Waser</LastName><ForeName>Beatrice</ForeName><Initials>B</Initials></Author><Author ValidYN="Y"><LastName>Reubi</LastName><ForeName>Jean-Claude</ForeName><Initials>JC</Initials></Author><Author ValidYN="Y"><LastName>Maecke</LastName><ForeName>Helmut R</ForeName><Initials>HR</Initials></Author></AuthorList><Language>eng</Language><PublicationTypeList><PublicationType>Comparative Study</PublicationType><PublicationType>Evaluation Studies</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>Indium Radioisotopes</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Radiopharmaceuticals</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Receptors, Bombesin</NameOfSubstance></Chemical><Chemical><RegistryNumber>0</RegistryNumber><NameOfSubstance>Tumor Markers, Biological</NameOfSubstance></Chemical><Chemical><RegistryNumber>7440-26-8</RegistryNumber><NameOfSubstance>Technetium</NameOfSubstance></Chemical><Chemical><RegistryNumber>PX9AZU7QPK</RegistryNumber><NameOfSubstance>Bombesin</NameOfSubstance></Chemical></ChemicalList><CitationSubset>IM</CitationSubset><MeshHeadingList><MeshHeading><DescriptorName MajorTopicYN="N">Animals</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Bombesin</DescriptorName><QualifierName MajorTopicYN="Y">analogs & derivatives</QualifierName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="Y">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="Y">Disease Models, Animal</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Drug Delivery Systems</DescriptorName><QualifierName MajorTopicYN="Y">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Female</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Humans</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Indium Radioisotopes</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Isotope Labeling</DescriptorName><QualifierName MajorTopicYN="N">methods</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Male</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Metabolic Clearance Rate</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Mice, Nude</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Radiopharmaceuticals</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Rats, Inbred Lew</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Receptors, Bombesin</DescriptorName><QualifierName MajorTopicYN="Y">metabolism</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Reproducibility of Results</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Sensitivity and Specificity</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Species Specificity</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Technetium</DescriptorName><QualifierName MajorTopicYN="N">diagnostic use</QualifierName><QualifierName MajorTopicYN="N">pharmacokinetics</QualifierName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tissue Distribution</DescriptorName></MeshHeading><MeshHeading><DescriptorName MajorTopicYN="N">Tumor Markers, Biological</DescriptorName><QualifierName MajorTopicYN="N">metabolism</QualifierName></MeshHeading></MeshHeadingList></MedlineCitation><PubmedData><History><PubMedPubDate 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