About: Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450.     Goto   Sponge   NotDistinct   Permalink

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  • 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 (en)
Title
  • Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450.
  • Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. (en)
skos:prefLabel
  • Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450.
  • Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. (en)
skos:notation
  • RIV/61989592:15110/09:00009616!RIV10-MSM-15110___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(KAN200200651), Z(AV0Z50040507), Z(AV0Z50040702), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika
  • 5
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 319893
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15110/09:00009616
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Carboplatin; cisplatin; cytochromes P450; human liver microsomes; oxaliplatin; transplatin; transplatin derivatives. (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [37F9BE2694B6]
http://linked.open...i/riv/nazevZdroje
  • Anti-Cancer Drugs
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 20
http://linked.open...iv/tvurceVysledku
  • Brabec, V.
  • Anzenbacher, Pavel
  • Anzenbacherová, Eva
  • Mašek, Vlastimil
  • Machová, M.
http://linked.open...n/vavai/riv/zamer
issn
  • 0959-4973
number of pages
http://localhost/t...ganizacniJednotka
  • 15110
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