title: Activation of anti-reverse transcriptase nucleotide analogs by nucleoside diphosphate kinase: improvement by alpha-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 (BH3-) or a thio (SH) group on the alpha-phosphate. Both the alpha-Rp-borano derivatives of AZT and d4T improved phosphorylation by NDP kinase, inhibition of reverse transcription as well as stability of alpha-borano nonophosphate derivatives in terminated viral DNA chain.
authors.affiliation: Unité de Régulation Enzymatique des Activités Cellulaires, CNRS URA 1773, Institut Pasteur, Paris, France.
authors.forename: B
authors.initials: B
authors.lastname: Schneider
authors.forename: P
authors.initials: P
authors.lastname: Meyer
authors.forename: S
authors.initials: S
authors.lastname: Sarfati
authors.forename: L
authors.initials: L
authors.lastname: Mulard
authors.forename: C
authors.initials: C
authors.lastname: Guerreiro
authors.forename: J
authors.initials: J
authors.lastname: Boretto
authors.forename: J
authors.initials: J
authors.lastname: Janin
authors.forename: M
authors.initials: M
authors.lastname: Véron
authors.forename: D
authors.initials: D
authors.lastname: Deville-Bonne
authors.forename: B
authors.initials: B
authors.lastname: Canard
mesh_terms: D019380:Anti-HIV Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D001711:Biotransformation; D001896:Boron Compounds / Q000493:pharmacokinetics* / Q000494:pharmacology; D015224:Dideoxynucleosides / Q000493:pharmacokinetics* / Q000494:pharmacology; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D008958:Models, Molecular; D009701:Nucleoside-Diphosphate Kinase / Q000378:metabolism*; D018894:Reverse Transcriptase Inhibitors / Q000493:pharmacokinetics* / Q000494:pharmacology; D018119:Stavudine / Q000031:analogs & derivatives; D013329:Structure-Activity Relationship; D015215:Zidovudine / Q000031:analogs & derivatives
chemical_list: D019380:Anti-HIV Agents; D001896:Boron Compounds; D015224:Dideoxynucleosides; D018894:Reverse Transcriptase Inhibitors; D015215:Zidovudine; D018119:Stavudine; D009701:Nucleoside-Diphosphate Kinase; D054303:HIV Reverse Transcriptase