The Sound of Evolution
Zidovudine
Mechanism of action:
Zidovudine is a nucleoside reverse transcriptase inhibitor and a thymidine analog. After entering host cells, it undergoes sequential phosphorylation by intracellular kinases to form the active metabolite zidovudine-5'-triphosphate. Zidovudine-5'-triphosphate competes with dTTP and is incorporated into newly synthesized viral DNA by HIV reverse transcriptase. Because zidovudine lacks a 3'-OH group, its incorporation causes termination of viral DNA synthesis.
Reference(s):
1. De Clercq E et al. (1994). HIV resistance to reverse transcriptase inhibitors. Biochem Pharmacol.
2. Yarchoan R et al. (1988). AIDS therapies. Sci Am.
3. Connor EM et al. (1994). Reduction of maternal-infant transmission of human immunodeficiency virus type 1 with zidovudine treatment. Pediatric AIDS Clinical Trials Group Protocol 076 Study Group. N Engl J Med.