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Design and evaluation of novel radiolabelled VIP derivatives for tumour targeting.

Identifieur interne : 000799 ( Main/Exploration ); précédent : 000798; suivant : 000800

Design and evaluation of novel radiolabelled VIP derivatives for tumour targeting.

Auteurs : RBID : pubmed:23564795

English descriptors

Abstract

Vasoactive intestinal peptide (VIP) receptors are overexpressed in a broad variety of tumours. For the detection of these tumours, novel chemically modified and shortened VIP derivatives were designed.

PubMed: 23564795

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Le document en format XML

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<title xml:lang="en">Design and evaluation of novel radiolabelled VIP derivatives for tumour targeting.</title>
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<name sortKey="Rangger, Christine" uniqKey="Rangger C">Christine Rangger</name>
<affiliation wicri:level="1">
<nlm:affiliation>Clinical Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck, Austria.</nlm:affiliation>
<country xml:lang="fr">Autriche</country>
<wicri:regionArea>Clinical Department of Nuclear Medicine, Innsbruck Medical University, Innsbruck</wicri:regionArea>
</affiliation>
</author>
<author>
<name sortKey="Helbok, Anna" uniqKey="Helbok A">Anna Helbok</name>
</author>
<author>
<name sortKey="Ocak, Meltem" uniqKey="Ocak M">Meltem Ocak</name>
</author>
<author>
<name sortKey="Radolf, Thorsten" uniqKey="Radolf T">Thorsten Radolf</name>
</author>
<author>
<name sortKey="Andreae, Fritz" uniqKey="Andreae F">Fritz Andreae</name>
</author>
<author>
<name sortKey="Virgolini, Irene J" uniqKey="Virgolini I">Irene J Virgolini</name>
</author>
<author>
<name sortKey="Von Guggenberg, Elisabeth" uniqKey="Von Guggenberg E">Elisabeth Von Guggenberg</name>
</author>
<author>
<name sortKey="Decristoforo, Clemens" uniqKey="Decristoforo C">Clemens Decristoforo</name>
</author>
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<date when="2013">2013</date>
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<term>Animals</term>
<term>Binding, Competitive</term>
<term>CHO Cells</term>
<term>Carcinoma, Pancreatic Ductal (metabolism)</term>
<term>Carcinoma, Pancreatic Ductal (radionuclide imaging)</term>
<term>Carcinoma, Pancreatic Ductal (radiotherapy)</term>
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<term>Pancreatic Neoplasms (metabolism)</term>
<term>Pancreatic Neoplasms (radionuclide imaging)</term>
<term>Pancreatic Neoplasms (radiotherapy)</term>
<term>Peptide Fragments (metabolism)</term>
<term>Peptide Fragments (pharmacokinetics)</term>
<term>Radiopharmaceuticals (diagnostic use)</term>
<term>Receptors, Vasoactive Intestinal Peptide (metabolism)</term>
<term>Tissue Distribution</term>
<term>Vasoactive Intestinal Peptide (metabolism)</term>
<term>Vasoactive Intestinal Peptide (pharmacokinetics)</term>
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<term>Pancreatic Neoplasms</term>
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<term>Receptors, Vasoactive Intestinal Peptide</term>
<term>Vasoactive Intestinal Peptide</term>
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<term>Peptide Fragments</term>
<term>Vasoactive Intestinal Peptide</term>
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<term>Carcinoma, Pancreatic Ductal</term>
<term>Pancreatic Neoplasms</term>
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<keywords scheme="MESH" qualifier="radiotherapy" xml:lang="en">
<term>Carcinoma, Pancreatic Ductal</term>
<term>Pancreatic Neoplasms</term>
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<term>Animals</term>
<term>Binding, Competitive</term>
<term>CHO Cells</term>
<term>Cells, Cultured</term>
<term>Cricetinae</term>
<term>Drug Design</term>
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<term>Humans</term>
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<front>
<div type="abstract" xml:lang="en">Vasoactive intestinal peptide (VIP) receptors are overexpressed in a broad variety of tumours. For the detection of these tumours, novel chemically modified and shortened VIP derivatives were designed.</div>
</front>
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<pubmed>
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<PMID Version="1">23564795</PMID>
<DateCreated>
<Year>2013</Year>
<Month>04</Month>
<Day>08</Day>
</DateCreated>
<DateCompleted>
<Year>2013</Year>
<Month>06</Month>
<Day>11</Day>
</DateCompleted>
<Article PubModel="Print">
<Journal>
<ISSN IssnType="Electronic">1791-7530</ISSN>
<JournalIssue CitedMedium="Internet">
<Volume>33</Volume>
<Issue>4</Issue>
<PubDate>
<Year>2013</Year>
<Month>Apr</Month>
</PubDate>
</JournalIssue>
<Title>Anticancer research</Title>
<ISOAbbreviation>Anticancer Res.</ISOAbbreviation>
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<ArticleTitle>Design and evaluation of novel radiolabelled VIP derivatives for tumour targeting.</ArticleTitle>
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<MedlinePgn>1537-46</MedlinePgn>
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<AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">Vasoactive intestinal peptide (VIP) receptors are overexpressed in a broad variety of tumours. For the detection of these tumours, novel chemically modified and shortened VIP derivatives were designed.</AbstractText>
<AbstractText Label="MATERIALS AND METHODS" NlmCategory="METHODS">1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-derivatised VIP analogues were radiolabelled with (111)In and in vitro and in vivo behaviour was evaluated using stability and internalisation assays, as well as an initial biodistribution study.</AbstractText>
<AbstractText Label="RESULTS" NlmCategory="RESULTS">Radiolabelling of the VIP analogues resulted in high radiochemical yields, without need for further purification steps. Stability of the VIP derivatives was variable and cell uptake studies in VIP receptor-positive cell lines revealed that only a limited number of derivatives were internalised. In the tumour mouse model, no specific tumour targeting was shown.</AbstractText>
<AbstractText Label="CONCLUSION" NlmCategory="CONCLUSIONS">Since the tested VIP derivatives exhibited impaired in vitro and in vivo characteristics alternative modifications to increase their stability while retaining receptor affinity should be considered to enable the use of synthetic VIP analogues for tumour targeting.</AbstractText>
</Abstract>
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<ForeName>Christine</ForeName>
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<Language>eng</Language>
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<PublicationType>Research Support, Non-U.S. Gov't</PublicationType>
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