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Statements

Subject Item
n2:RIV%2F61989592%3A15110%2F09%3A00009616%21RIV10-MSM-15110___
rdf:type
skos:Concept n18:Vysledek
dcterms:description
Interaction of nine human hepatic cytochromes P450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4) with six platinum complexes was studied using pooled human microsomes. The compounds used were cisplatin, oxaliplatin, carboplatin, transplatin, and trans-[PtCl2(NH3) (Am)], where Am=2-methylbutylamine or sec-butylamine. No significant inhibition of all CYP activities by carboplatin was observed. With cisplatin and oxaliplatin, a minor inhibition of CYP2C9 enzyme (75% of control at 400 miromol/l of these complexes) was seen; cisplatin also inhibited slightly the CYP2B6 activity (85% of control). With respect to plasma levels of cisplatin obtained in clinical applications, these effects are probably not important. In contrast, clinically ineffective transplatin, inhibited the CYP2B6 as well as CYP2C9 activities significantly (to 50-35% of control at 100 micromol/l); also, an inhibition of CYP2E1 activity was found here (to 70% at 100 micromol/l). Two other derivatives of tran Interaction of nine human hepatic cytochromes P450 (CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4) with six platinum complexes was studied using pooled human microsomes. The compounds used were cisplatin, oxaliplatin, carboplatin, transplatin, and trans-[PtCl2(NH3) (Am)], where Am=2-methylbutylamine or sec-butylamine. No significant inhibition of all CYP activities by carboplatin was observed. With cisplatin and oxaliplatin, a minor inhibition of CYP2C9 enzyme (75% of control at 400 miromol/l of these complexes) was seen; cisplatin also inhibited slightly the CYP2B6 activity (85% of control). With respect to plasma levels of cisplatin obtained in clinical applications, these effects are probably not important. In contrast, clinically ineffective transplatin, inhibited the CYP2B6 as well as CYP2C9 activities significantly (to 50-35% of control at 100 micromol/l); also, an inhibition of CYP2E1 activity was found here (to 70% at 100 micromol/l). Two other derivatives of tran
dcterms:title
Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450.
skos:prefLabel
Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450.
skos:notation
RIV/61989592:15110/09:00009616!RIV10-MSM-15110___
n3:aktivita
n6:Z n6:P
n3:aktivity
P(KAN200200651), Z(AV0Z50040507), Z(AV0Z50040702), Z(MSM6198959216)
n3:cisloPeriodika
5
n3:dodaniDat
n16:2010
n3:domaciTvurceVysledku
n11:8321124 n11:7271859 n11:2899183
n3:druhVysledku
n9:J
n3:duvernostUdaju
n4:S
n3:entitaPredkladatele
n14:predkladatel
n3:idSjednocenehoVysledku
319893
n3:idVysledku
RIV/61989592:15110/09:00009616
n3:jazykVysledku
n17:eng
n3:klicovaSlova
Carboplatin; cisplatin; cytochromes P450; human liver microsomes; oxaliplatin; transplatin; transplatin derivatives.
n3:klicoveSlovo
n7:Carboplatin n7:transplatin n7:transplatin%20derivatives. n7:oxaliplatin n7:cisplatin n7:cytochromes%20P450 n7:human%20liver%20microsomes
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[37F9BE2694B6]
n3:nazevZdroje
Anti-Cancer Drugs
n3:obor
n15:FR
n3:pocetDomacichTvurcuVysledku
3
n3:pocetTvurcuVysledku
5
n3:projekt
n10:KAN200200651
n3:rokUplatneniVysledku
n16:2009
n3:svazekPeriodika
20
n3:tvurceVysledku
Anzenbacherová, Eva Brabec, V. Machová, M. Anzenbacher, Pavel Mašek, Vlastimil
n3:zamer
n8:MSM6198959216 n8:AV0Z50040507 n8:AV0Z50040702
s:issn
0959-4973
s:numberOfPages
7
n19:organizacniJednotka
15110