Dynamics of antifolate transport via the reduced folate carrier and the membrane folate receptor in murine leukaemia cells in vitro and in vivo
作者： Robert Mauritz , Godefridus J. Peters , Ietje Kathmann , Habte Teshale , Paul Noordhuis
DOI: 10.1007/S00280-008-0683-0
关键词:
摘要: Murine L1210 leukaemia cells expressing either the reduced folate carrier (RFC) or membrane receptor (MFR) were studied in vitro and vivo to assess dynamics of transport two catego- ries antifolates; folate-based inhibitors dihydrofolate reductase (methotrexate, edatrexate, aminopterin, PT523, PT644) thymidylate synthase (TS) (CB3717, ral- titrexed, plevitrexed (BGC9331), pemetrexed GW1843). The potency situ inhibition TS was used as an endpoint analyze RFC/ MFR-membrane these antifolates. Both for L1210-RFC L1210-MFR cells, closely correlated with increasing aYni- ties transporters antifolates (r =0 .64, P < 0.05 r = i0.65, 0.05, respectively). Within group which MFR had a low binding aYnity, those that ability become polyglutamy- lated, more potent activity than non-polyglutamatable In metho- trexate, raltitrexed assessed bearing mice fed standard folate-deWcient chow. Die- tary depletion signiWcantly MTD methotrexate (sevenfold), edatrexate raltitr- exed (50-fold) (150-fold). Based on increased life spans, antitumor eVects markedly better chow (ILS: 455 544%, respectively) 213 263%, No therapeutic observed condition, may be consistent aYnity MFR. Irrespective diet status, inactive against both mice, due high circulating plasma thymidine levels. Collectively, this study underscores modulation die- status can provide basis within ther- apeutic eVect further improved.
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