ACTIVATION OF ANTI-REVERSE TRANSCRIPTASE NUCLEOTIDE ANALOGS BY NUCLEOSIDE DIPHOSPHATE KINASE: IMPROVEMENT BY α-BORANOPHOSPHATE SUBSTITUTION

Abstract

Nucleoside activation by nucleoside diphosphate kinase and inhibition of HIV-1 reverse transcriptase were studied comparatively for a new class of nucleoside analogs with a borano (BH⁻ ₃) or a thio (SH) group on the α-phosphate. Both the α-Rp-borano derivatives of AZT and d4T improved phosphorylation by NDP kinase, inhibition of reverse transcription as well as stability of α-borano monophosphate derivatives in terminated viral DNA chain.

ACKNOWLEDGMENT

This work was supported in part by grant from the Agence Nationale de la Recherche contre le SIDA.