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Statements

Subject Item
n2:RIV%2F61388971%3A_____%2F11%3A00360736%21RIV12-AV0-61388971
rdf:type
n11:Vysledek skos:Concept
dcterms: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.
dcterms:title
Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach
skos:prefLabel
Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach Ellipticine-aimed polymer-conjugated Auger electron emitter: multistage organelle targeting approach
skos:notation
RIV/61388971:_____/11:00360736!RIV12-AV0-61388971
n11:predkladatel
n12:ico%3A61388971
n3:aktivita
n16:P n16:Z
n3:aktivity
P(1M0505), P(GAP108/10/1560), P(GPP207/10/P054), P(IAAX00500803), Z(AV0Z40500505), Z(AV0Z50200510)
n3:cisloPeriodika
6
n3:dodaniDat
n10:2012
n3:domaciTvurceVysledku
n9:1130706 n9:9792155 n9:3227820
n3:druhVysledku
n14:J
n3:duvernostUdaju
n20:S
n3:entitaPredkladatele
n15:predkladatel
n3:idSjednocenehoVysledku
197298
n3:idVysledku
RIV/61388971:_____/11:00360736
n3:jazykVysledku
n7:eng
n3:klicovaSlova
ellipticine; drug delivery; radiotherapy
n3:klicoveSlovo
n17:drug%20delivery n17:radiotherapy n17:ellipticine
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[8E7AF45945FB]
n3:nazevZdroje
Bioconjugate Chemistry
n3:obor
n8:CD
n3:pocetDomacichTvurcuVysledku
3
n3:pocetTvurcuVysledku
8
n3:projekt
n5:GAP108%2F10%2F1560 n5:1M0505 n5:IAAX00500803 n5:GPP207%2F10%2FP054
n3:rokUplatneniVysledku
n10:2011
n3:svazekPeriodika
22
n3:tvurceVysledku
Hrubý, Martin Říhová, Blanka Sedláček, Ondřej Ulbrich, Karel Studenovský, Martin Kučka, Jan Větvička, David Kovář, Lubomír
n3:wos
000291568200024
n3:zamer
n18:AV0Z50200510 n18:AV0Z40500505
s:issn
1043-1802
s:numberOfPages
8
n13:doi
10.1021/bc200064v