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Statements

Subject Item
n2:RIV%2F68081707%3A_____%2F13%3A00399490%21RIV14-GA0-68081707
rdf:type
n4:Vysledek skos:Concept
dcterms:description
In order to shed light on the mechanism that underlies activity of bifunctional mononuclear Pt-II analogs of transplatin we examined in the present work a DNA binding mode of the analog of transplatin, namely trans-[Pt(CH3NH2)(2)Cl-2], in which NH3 groups were replaced only by a small, non-bulky-methylamine-ligand. This choice was made because we were interested to reveal the role of the bulkiness of the amines used to substitute NH3 in transplatin to produce antitumor-active Pt-II drug. The results indicate that trans-[Pt(CH3NH2)(2)Cl-2] forms a markedly higher amount of more distorting intrastrand cross-links than transplatin which forms in DNA preferentially less distorting and persisting monofunctional adducts. Also importantly, the accumulation of trans-[Pt(CH3NH2)(2)Cl-2] in tumor cells was considerably greater than that of transplatin and cisplatin In order to shed light on the mechanism that underlies activity of bifunctional mononuclear Pt-II analogs of transplatin we examined in the present work a DNA binding mode of the analog of transplatin, namely trans-[Pt(CH3NH2)(2)Cl-2], in which NH3 groups were replaced only by a small, non-bulky-methylamine-ligand. This choice was made because we were interested to reveal the role of the bulkiness of the amines used to substitute NH3 in transplatin to produce antitumor-active Pt-II drug. The results indicate that trans-[Pt(CH3NH2)(2)Cl-2] forms a markedly higher amount of more distorting intrastrand cross-links than transplatin which forms in DNA preferentially less distorting and persisting monofunctional adducts. Also importantly, the accumulation of trans-[Pt(CH3NH2)(2)Cl-2] in tumor cells was considerably greater than that of transplatin and cisplatin
dcterms:title
Activation of trans geometry in bifunctional mononuclear platinum complexes by a non-bulky methylamine ligand Activation of trans geometry in bifunctional mononuclear platinum complexes by a non-bulky methylamine ligand
skos:prefLabel
Activation of trans geometry in bifunctional mononuclear platinum complexes by a non-bulky methylamine ligand Activation of trans geometry in bifunctional mononuclear platinum complexes by a non-bulky methylamine ligand
skos:notation
RIV/68081707:_____/13:00399490!RIV14-GA0-68081707
n4:predkladatel
n5:ico%3A68081707
n7:aktivita
n16:Z n16:I n16:S n16:P
n7:aktivity
I, P(EE2.3.20.0057), P(GA13-08273S), P(GAP301/10/0598), S, Z(AV0Z50040702)
n7:cisloPeriodika
SEP2013
n7:dodaniDat
n9:2014
n7:domaciTvurceVysledku
n11:3900991 n11:4571932 n11:5105307 n11:7988346 n11:6854974
n7:druhVysledku
n19:J
n7:duvernostUdaju
n14:S
n7:entitaPredkladatele
n17:predkladatel
n7:idSjednocenehoVysledku
59392
n7:idVysledku
RIV/68081707:_____/13:00399490
n7:jazykVysledku
n8:eng
n7:klicovaSlova
HETEROCYCLIC AMINE LIGAND; INTERSTRAND CROSS-LINKS; DNA-BINDING MODE
n7:klicoveSlovo
n10:DNA-BINDING%20MODE n10:INTERSTRAND%20CROSS-LINKS n10:HETEROCYCLIC%20AMINE%20LIGAND
n7:kodStatuVydavatele
US - Spojené státy americké
n7:kontrolniKodProRIV
[36ABD2572721]
n7:nazevZdroje
Journal of Inorganic Biochemistry
n7:obor
n12:BO
n7:pocetDomacichTvurcuVysledku
5
n7:pocetTvurcuVysledku
7
n7:projekt
n15:EE2.3.20.0057 n15:GAP301%2F10%2F0598 n15:GA13-08273S
n7:rokUplatneniVysledku
n9:2013
n7:svazekPeriodika
126
n7:tvurceVysledku
Kašpárková, Jana Gibson, D. Nováková, Olga Novohradský, Vojtěch Frýbortová, M. Brabec, Viktor Štěpánková, Jana
n7:wos
000322942400007
n7:zamer
n20:AV0Z50040702
s:issn
0162-0134
s:numberOfPages
9
n18:doi
10.1016/j.jinorgbio.2013.05.009