Activation of anti-reverse transcriptase nucleotide analogs by nucleoside diphosphate kinase: improvement by alpha-boranophosphate substitution.
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.
Schneider
B
B
Unité de Régulation Enzymatique des Activités Cellulaires, CNRS URA 1773, Institut Pasteur, Paris, France.
Meyer
P
P
Sarfati
S
S
Mulard
L
L
Guerreiro
C
C
Boretto
J
J
Janin
J
J
Véron
M
M
Deville-Bonne
D
D
Canard
B
B
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
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