DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

1. Triphosphate competes
with native nucleotides
(shown is zidovudine 5 –triphosphate)
O –
O –
O –
O P O P O P HO
O O O
N – N + N
O
O
HN
O
N
CH 3
Daughter DNA strand
Parent RNA strand
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CHAPTER 59
2. Incorporation
and chain
termination
O
HN
O
N
Zidovudine
CH 3
O
N – N + N
Didanosine Stavudine Zalcitabine Lamivudine
O O O
CH 3
H
HN
HN N
N
N
N N
O
O N
HO CH 2 HO CH 2 HO CH 2
O
O
O
O
P
O
HIV reverse transcriptase
NH 2
NH 2
CH 3
N
N
O N
O N O CH 2
HO
O
5 2
H S
H
OH
ANTIRETROVIRAL AGENTS AND TREATMENT OF HIV INFECTION
N 3
Abacavir Tenofovir disoproxil Emtricitabine
HN
N
NH 2
CH 2
H 2 N
N
N
O
H 2 N
N
N
N
N
N
N
O
O
O P O O O
F
N
O
S
OH
CH 2 OH
CH 3
O O O
O
Figure 59–2. Structures and mechanism of nucleoside and nucleotide reverse transcriptase inhibitors.