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Statements

Subject Item
n2:RIV%2F61388963%3A_____%2F13%3A00396057%21RIV14-GA0-61388963
rdf:type
n10:Vysledek skos:Concept
dcterms:description
Aim: 6-Chloropurines substituted at position 9 with bicyclic skeletons represent promising chemotherapeutic agents. We explored the metabolism and membrane transport of 9-norbornyl-6-chloropurine (NCP) aiming to understand its mechanism of action. Materials and Methods: The metabolism of NCP was studied in vitro in whole cells (CCRF-CEM), cellular extracts, subcellular fractions and purified enzymes. Transport experiments were conducted in Caco-2 cell monolayers. Results: Three metabolites were identified, a glutathione conjugate (NCP-GS), NCP-cysteinylglycine and NCP-cysteine. Both glutathione-S-transferase inhibition and glutathione (GSH) depletion prevented metabolite formation and increased the cytotoxicity of NCP. Transepithelial transport (Caco-2) indicated good permeability, with P-app (12.6+/-0.3) x10(-5) cm/s. Importantly, the drug induced glutathione depletion in treated cells and affected the activity of several GSH-dependent enzymes. Conclusion: The novel nucleoside analog NCP represents a promising orally available antileukemic agent, acting through lowering of GSH levels in tumor cells. Aim: 6-Chloropurines substituted at position 9 with bicyclic skeletons represent promising chemotherapeutic agents. We explored the metabolism and membrane transport of 9-norbornyl-6-chloropurine (NCP) aiming to understand its mechanism of action. Materials and Methods: The metabolism of NCP was studied in vitro in whole cells (CCRF-CEM), cellular extracts, subcellular fractions and purified enzymes. Transport experiments were conducted in Caco-2 cell monolayers. Results: Three metabolites were identified, a glutathione conjugate (NCP-GS), NCP-cysteinylglycine and NCP-cysteine. Both glutathione-S-transferase inhibition and glutathione (GSH) depletion prevented metabolite formation and increased the cytotoxicity of NCP. Transepithelial transport (Caco-2) indicated good permeability, with P-app (12.6+/-0.3) x10(-5) cm/s. Importantly, the drug induced glutathione depletion in treated cells and affected the activity of several GSH-dependent enzymes. Conclusion: The novel nucleoside analog NCP represents a promising orally available antileukemic agent, acting through lowering of GSH levels in tumor cells.
dcterms:title
9-Norbornyl-6-chloropurine Is a Novel Antileukemic Compound Interacting with Cellular GSH 9-Norbornyl-6-chloropurine Is a Novel Antileukemic Compound Interacting with Cellular GSH
skos:prefLabel
9-Norbornyl-6-chloropurine Is a Novel Antileukemic Compound Interacting with Cellular GSH 9-Norbornyl-6-chloropurine Is a Novel Antileukemic Compound Interacting with Cellular GSH
skos:notation
RIV/61388963:_____/13:00396057!RIV14-GA0-61388963
n10:predkladatel
n11:ico%3A61388963
n3:aktivita
n16:P n16:I
n3:aktivity
I, P(GAP303/11/1297)
n3:cisloPeriodika
8
n3:dodaniDat
n7:2014
n3:domaciTvurceVysledku
n5:7359608 n5:9822666 n5:4843878 n5:6298036 n5:8571325 n5:2131447 n5:5104998 n5:7989776
n3:druhVysledku
n17:J
n3:duvernostUdaju
n18:S
n3:entitaPredkladatele
n12:predkladatel
n3:idSjednocenehoVysledku
120012
n3:idVysledku
RIV/61388963:_____/13:00396057
n3:jazykVysledku
n9:eng
n3:klicovaSlova
Substituted 6-chloropurines; carbocyclic nucleoside analogs; glutathione-S-transferase; glutathione depletion
n3:klicoveSlovo
n4:glutathione%20depletion n4:Substituted%206-chloropurines n4:glutathione-S-transferase n4:carbocyclic%20nucleoside%20analogs
n3:kodStatuVydavatele
GR - Řecká republika
n3:kontrolniKodProRIV
[BB457E96308E]
n3:nazevZdroje
Anticancer Research
n3:obor
n8:FD
n3:pocetDomacichTvurcuVysledku
8
n3:pocetTvurcuVysledku
9
n3:projekt
n15:GAP303%2F11%2F1297
n3:rokUplatneniVysledku
n7:2013
n3:svazekPeriodika
33
n3:tvurceVysledku
Dvořáková, Alexandra Elbert, Tomáš Mertlíková-Kaiserová, Helena Plačková, Pavla Nencka, Radim Rozumová, N. Votruba, Ivan Šála, Michal Hřebabecký, Hubert
n3:wos
000322559300025
s:issn
0250-7005
s:numberOfPages
6