Mechanistic studies to understand the inhibition of wild type and mutant HIV-1 reverse transcriptase by Carbovir-triphosphate.
Abacavir (1592U89) has recently been approved by the FDA for treatment of HIV infection. Transient kinetic studies were carried out to better understand the interaction of the active metabolite of Abacavir (Carbovir-triphosphate) with wild type and mutant HIV-1 reverse transcriptase. Some of the data is summarized and used as a basis for discussion of inhibition by CBVTP and previously studied nucleoside analogs.
Ray
A S
AS
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, Connecticut 06520-8066, USA.
Anderson
K S
KS
D019380:Anti-HIV Agents / Q000494:pharmacology*; D017931:DNA Primers / Q000737:chemistry / Q000378:metabolism; D003848:Deoxyguanine Nucleotides / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D012313:RNA / Q000737:chemistry / Q000378:metabolism; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology*; D013698:Templates, Genetic; D006160:Guanosine Triphosphate
D019380:Anti-HIV Agents; D017931:DNA Primers; D003848:Deoxyguanine Nucleotides; D054303:HIV Reverse Transcriptase; D012313:RNA; D018894:Reverse Transcriptase Inhibitors; C034477:RNA primers; C066928:carbovir triphosphate; D006160:Guanosine Triphosphate