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Improved in vivo antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice

Improved in vivo antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice

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KAPUVÁRI, Bence, Rózsa HEGEDÜS, Ákos SCHULCZ, Marilena MANEA, József TÓVÁRI, Alexandra GACS, Borbála VINCZE, Gábor MEZŐ, 2016. Improved in vivo antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice. In: Investigational New Drugs. 34(4), pp. 416-423. ISSN 0167-6997. eISSN 1573-0646

@article{Kapuvari2016Impro-39823, title={Improved in vivo antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice}, year={2016}, doi={10.1007/s10637-016-0354-7}, number={4}, volume={34}, issn={0167-6997}, journal={Investigational New Drugs}, pages={416--423}, author={Kapuvári, Bence and Hegedüs, Rózsa and Schulcz, Ákos and Manea, Marilena and Tóvári, József and Gacs, Alexandra and Vincze, Borbála and Mező, Gábor} }

<rdf:RDF xmlns:rdf="http://www.w3.org/1999/02/22-rdf-syntax-ns#" xmlns:bibo="http://purl.org/ontology/bibo/" xmlns:dc="http://purl.org/dc/elements/1.1/" xmlns:dcterms="http://purl.org/dc/terms/" xmlns:xsd="http://www.w3.org/2001/XMLSchema#" > <rdf:Description rdf:about="https://kops.uni-konstanz.de/rdf/resource/123456789/39823"> <dc:date rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2017-08-10T09:18:56Z</dc:date> <dc:contributor>Kapuvári, Bence</dc:contributor> <dc:contributor>Schulcz, Ákos</dc:contributor> <dcterms:issued>2016</dcterms:issued> <dc:creator>Mező, Gábor</dc:creator> <dcterms:abstract xml:lang="eng">Compared to classical chemotherapy, peptide-based drug targeting is a promising therapeutic approach for cancer, which can provide increased selectivity and decreased side effects to anticancer drugs. Among various homing devices, gonadotropin-releasing hormone-III (GnRH-III) peptide represents a suitable targeting moiety, in particular in the treatment of hormone independent tumors that highly express GnRH receptors (e.g. colon carcinoma). We have previously shown that GnRH-III[(4)Lys(Ac),(8)Lys(Dau = Aoa)] bioconjugate, in which daunorubicin was attached via oxime linkage to the (8)Lys of a GnRH-III derivative, exerted significant in vivo antitumor effect on subcutaneously developed HT-29 colon tumor. In contrast, results of the study reported here indicated that this compound was not active on an orthotopically developed tumor. However, if Lys in position 4 was acylated with butyric acid instead of acetic acid, the resulting bioconjugate GnRH-III[(4)Lys(Bu),(8)Lys(Dau = Aoa)] had significant tumor growth inhibitory effect. Furthermore, it prevented tumor neovascularization, without detectable side effects. Nevertheless, the development of metastases could not be inhibited by the bioconjugate; therefore, its application in combination with a metastasis preventive agent might be necessary in order to achieve complete tumor remission. In spite of this result, the treatment with GnRH-III[(4)Lys(Bu),(8)Lys(Dau = Aoa)] bioconjugate proved to have significant benefits over the administration of free daunorubicin, which was used at the maximum tolerated dose.</dcterms:abstract> <dc:language>eng</dc:language> <dc:contributor>Manea, Marilena</dc:contributor> <dc:creator>Schulcz, Ákos</dc:creator> <dc:contributor>Vincze, Borbála</dc:contributor> <dc:creator>Kapuvári, Bence</dc:creator> <dc:contributor>Hegedüs, Rózsa</dc:contributor> <dc:creator>Hegedüs, Rózsa</dc:creator> <bibo:uri rdf:resource="https://kops.uni-konstanz.de/handle/123456789/39823"/> <dc:contributor>Gacs, Alexandra</dc:contributor> <dcterms:title>Improved in vivo antitumor effect of a daunorubicin - GnRH-III bioconjugate modified by apoptosis inducing agent butyric acid on colorectal carcinoma bearing mice</dcterms:title> <dc:creator>Gacs, Alexandra</dc:creator> <dcterms:available rdf:datatype="http://www.w3.org/2001/XMLSchema#dateTime">2017-08-10T09:18:56Z</dcterms:available> <dc:creator>Manea, Marilena</dc:creator> <dc:contributor>Mező, Gábor</dc:contributor> <dc:creator>Vincze, Borbála</dc:creator> <dc:contributor>Tóvári, József</dc:contributor> <dc:creator>Tóvári, József</dc:creator> <dcterms:rights rdf:resource="http://nbn-resolving.de/urn:nbn:de:bsz:352-20150914100631302-4485392-8"/> </rdf:Description> </rdf:RDF>

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