DEOXYCYTIDINE DEAMINASE-RESISTANT FORM IS THE ACTIVE FORM OF +/-2',3'-DIDEOXY-3'-THIACYTIDINE (+/- SDDC) FOR THE INHIBITION OF HEPATITIS B VIRUS (HBV) AND HUMAN IMMUNODEFICIENCY VIRUSES (MEETING ABSTRACT)

Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

Proc Annu Meet Am Assoc Cancer Res; 33:A2385 1992. Unique Identifier : AIDSLINE ICDB/92685587
Chang CN; Doong SL; Zhou JH; Skalski V; Chu CK; Cheng YC; Dept. of Pharmacology, Yale Univ., New Haven, CT 06510

Abstract: In culture, +/-SddC was found to have potent activity against HIV as well as human HBV. The -form (-SddC), which is resistant to deoxycytidine deaminase, was found to be the more active antiviral stereo isomer and less toxic than the +form (+SddC) in terms of anti-cell growth and antimitochondrial DNA synthesis. The -form could be phosphorylated by cytoplasmic CdR kinase to SddCMP, which is subsequently converted to -SddCDP and -SddCTP. SddCTP is more potent than +SddCTP in inhibiting HBV replication, and they have approx equal potency for the inhibition of HIV-associated reverse transcriptase. +SddCTP and SddCTP exhibited differential inhibitions on each of the human DNA polymerases alpha, beta and gamma, but not DNA polymerase delta, which was not affected by these inhibitors.

Keywords: DNA Polymerases/METABOLISM Hepatitis B Virus/DRUG EFFECTS/PHYSIOLOGY HIV/*DRUG EFFECTS/PHYSIOLOGY Nucleoside Deaminases/METABOLISM/*PHARMACOLOGY Phosphorylation RNA-Directed DNA Polymerase Virus Replication Zalcitabine/*PHARMACOLOGY ABSTRACT
921230
M92C5366

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