ENANTIOMERIC SPECIFICITY OF CARBOVIR TRANSPORT (MEETING ABSTRACT) NLM AIDSLINE Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

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ENANTIOMERIC SPECIFICITY OF CARBOVIR TRANSPORT (MEETING ABSTRACT)

Proc Annu Meet Am Assoc Cancer Res; 33:A112 1992. Unique Identifier : AIDSLINE ICDB/92682646
Domin BA; Mahony WB; Daluge SM; Miller WH; Zimmerman TP; Div. of Experimental Therapy, Wellcome Res. Laboratories,; Research Triangle Park, NC 27709

Abstract: Carbovir (CBV), a guanosine analog with a carbocyclic sugar, inhibits the replication of human immunodeficiency virus. The transport of CBV enantiomers into human erythrocytes at 37 C was examined with a 'papaverine-stop' assay. The influx of both (-)CBV and (+)CBV occurred primarily (greater than 60%) via the nucleobase transporter with Vmax (pmol/sec/5 ul cells)/Km (mM) values of 17/0.12 and 150/1.9, respectively. The Km for each enantiomer was similar to its Ki as a competitive inhibitor of acyclovir influx via the nucleobase carrier. (-)CBV and (+)CBV also entered these cells via the nucleoside transporter. Although the affinities of both enantiomers for this carrier were similar (Km = 2 mM), the Vmax for (-)CBV was much higher than that for (+)CBV. We conclude that (1) (-)CBV and (+)CBV enter human erythrocytes primarily by the nucleobase carrier and secondarily by the nucleoside carrier and (2) these two carriers show different enantiomeric specificities for CBV.
Keywords: Acyclovir/BLOOD Antiviral Agents/*BLOOD Binding, Competitive Biological Transport Blood Proteins/METABOLISM Carrier Proteins/*METABOLISM Dideoxynucleosides/*BLOOD/PHARMACOLOGY Erythrocytes/*METABOLISM Human Kinetics Membrane Proteins/*METABOLISM Stereoisomers ABSTRACTKWDacyclovir/bloodantiviralagents/KWDbloodbinding,competitivebiologicaltransportbloodproteins/metabolismcarrierproteins/KWDmetabolismdideoxynucleosides/KWDblood/pharmacologyerythrocytes/KWDmetabolismhumankineticsmembraneproteins/KWDmetabolismstereoisomersabstract
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M9271109

Copyright © 1992 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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