About: Paclitaxel conjugation with the analog of the gonadotropin-releasing hormone as a targeting moiety

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An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	A new targeted conjugates in which paclitaxel was used as a cytostatic compound and an analog of the gonadotropin-releasing hormone (GnRH) as a targeting moiety were synthesized. The molecule of the peptide hormone GnRH was modified to allow its connection to paclitaxel via spacer. The conjugates were prepared as prodrugs using 2'-hydroxyl group of paclitaxel. 4-Maleimidobutyric acid and chloroacetic acid served as spacers. The structures of the prepared derivatives were analysed by NMR and HR-MS. The conjugates MP264 and MP265 were chosen and their antiproliferative effect was tested in the breast cancer cell line MCF-7 using the MTT test of cell viability and neutral red uptake test. In MCF-7 cells, conjugate MP265 showed higher antiproliferative effect than paclitaxel alone. Receptor saturation tests showed that the unconjugated peptide analog of GnRH decreased efficacy of conjugate MP265 in concentration- and time-dependent manner. A new targeted conjugates in which paclitaxel was used as a cytostatic compound and an analog of the gonadotropin-releasing hormone (GnRH) as a targeting moiety were synthesized. The molecule of the peptide hormone GnRH was modified to allow its connection to paclitaxel via spacer. The conjugates were prepared as prodrugs using 2'-hydroxyl group of paclitaxel. 4-Maleimidobutyric acid and chloroacetic acid served as spacers. The structures of the prepared derivatives were analysed by NMR and HR-MS. The conjugates MP264 and MP265 were chosen and their antiproliferative effect was tested in the breast cancer cell line MCF-7 using the MTT test of cell viability and neutral red uptake test. In MCF-7 cells, conjugate MP265 showed higher antiproliferative effect than paclitaxel alone. Receptor saturation tests showed that the unconjugated peptide analog of GnRH decreased efficacy of conjugate MP265 in concentration- and time-dependent manner. (en)
Title	Paclitaxel conjugation with the analog of the gonadotropin-releasing hormone as a targeting moiety Paclitaxel conjugation with the analog of the gonadotropin-releasing hormone as a targeting moiety (en)
skos:prefLabel	Paclitaxel conjugation with the analog of the gonadotropin-releasing hormone as a targeting moiety Paclitaxel conjugation with the analog of the gonadotropin-releasing hormone as a targeting moiety (en)
skos:notation	RIV/61389030:_____/11:00370667!RIV12-AV0-61389030
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(ME08070), S, Z(AV0Z50380511)
http://linked.open...iv/cisloPeriodika	1-2
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Dvořáková, Marcela Vaněk, Tomáš Přibylová, Marie
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	219385
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/11:00370667
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Paclitaxel; GnRH; Targeted drug delivery (en)
http://linked.open.../riv/klicoveSlovo	Paclitaxel GnRH Targeted drug delivery
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[235B437949AE]
http://linked.open...i/riv/nazevZdroje	International Journal of Pharmaceutics
http://linked.open...in/vavai/riv/obor	EI
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	6 (xsd:int)
http://linked.open...vavai/riv/projekt	Biotechnological production of Vaccinium bracteatum and evaluation of its biological activity
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	415
http://linked.open...iv/tvurceVysledku	Dvořáková, Marcela Vaněk, Tomáš Přibylová, Marie Hanusová, V. Nemethová, I. Skálová, L.
http://linked.open...ain/vavai/riv/wos	000293304900023
http://linked.open...n/vavai/riv/zamer	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy
issn	0378-5173
number of pages	6 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.ijpharm.2011.05.072

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