About: Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	We describe an ellipticine derivative-bound iodine-125 attached to hydrazide moieties containing poly[N-(2-hydroxypropyl)methacrylamide]. The system is completely stable at pH 7.4, while iodine-containing biologically active intercalator is released upon decrease of pH (25% intercalator released after 24 h incubation at pH 5.0—model of late endosomes). Both 2-N-(2-oxobutyl)-9-iodoellipticinium bromide and the noniodinated 2-N-(2-oxobutyl)ellipticinium bromide are potent intercalators, as proven by direct titration with DNA and ethidium displacement assay, and readily penetrate into cell nuclei, as proven by confocal microscopy. They retain chemotherapeutical antiproliferative properties of ellipticine against Raji, EL-4, and 4T1cells with IC50 in the range 0.27–8.8 μmol/L. Polymer conjugate of 2-N-(2-oxobutyl)-9-iodoellipticinium bromide is internalized into endosomes, releases active drug, possesses cytotoxic activity, and the drug accumulates in cell nuclei. We describe an ellipticine derivative-bound iodine-125 attached to hydrazide moieties containing poly[N-(2-hydroxypropyl)methacrylamide]. The system is completely stable at pH 7.4, while iodine-containing biologically active intercalator is released upon decrease of pH (25% intercalator released after 24 h incubation at pH 5.0—model of late endosomes). Both 2-N-(2-oxobutyl)-9-iodoellipticinium bromide and the noniodinated 2-N-(2-oxobutyl)ellipticinium bromide are potent intercalators, as proven by direct titration with DNA and ethidium displacement assay, and readily penetrate into cell nuclei, as proven by confocal microscopy. They retain chemotherapeutical antiproliferative properties of ellipticine against Raji, EL-4, and 4T1cells with IC50 in the range 0.27–8.8 μmol/L. Polymer conjugate of 2-N-(2-oxobutyl)-9-iodoellipticinium bromide is internalized into endosomes, releases active drug, possesses cytotoxic activity, and the drug accumulates in cell nuclei. (en)
Title	Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach (en)
skos:prefLabel	Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach (en)
skos:notation	RIV/61388971:_____/11:00360736!RIV12-AV0-61388971
http://linked.open...avai/predkladatel	Mikrobiologický ústav AV ČR, v.v.i.
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(1M0505), P(GAP108/10/1560), P(GPP207/10/P054), P(IAAX00500803), Z(AV0Z40500505), Z(AV0Z50200510)
http://linked.open...iv/cisloPeriodika	6
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Říhová, Blanka Kovář, Lubomír Větvička, David
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	Mikrobiologický ústav AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	197298
http://linked.open...ai/riv/idVysledku	RIV/61388971:_____/11:00360736
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	ellipticine; drug delivery; radiotherapy (en)
http://linked.open.../riv/klicoveSlovo	ellipticine radiotherapy drug delivery
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[8E7AF45945FB]
http://linked.open...i/riv/nazevZdroje	Bioconjugate Chemistry
http://linked.open...in/vavai/riv/obor	CD
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...vavai/riv/projekt	Center of targeted therapeutic drugs New generation of reductively biodegradable functionalized macroporous scaffolds for neural tissue engineering Polymeric micelles with metal ion – assembled core Multifunctional Polymer Systems with Cytostatic and Immunomobilizing Activities
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	22
http://linked.open...iv/tvurceVysledku	Hrubý, Martin Kovář, Lubomír Ulbrich, Karel Říhová, Blanka Studenovský, Martin Kučka, Jan Sedláček, Ondřej Větvička, David
http://linked.open...ain/vavai/riv/wos	000291568200024
http://linked.open...n/vavai/riv/zamer	Progresivní makromolekulární materiály a supramolekulární systémy: syntéza a studium vlastností, jevů a možností využití pro speciální aplikace a moderní technologie Microorganisms in Research and Biotechnology
issn	1043-1802
number of pages	8 (xsd:int)
http://bibframe.org/vocab/doi	10.1021/bc200064v
is http://linked.open...avai/riv/vysledek of	Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach

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