Affiliation:
1. Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic,
2. Institute of Biology and Medical Genetics, 1st Faculty of Medicine and General Teaching Hospital, Charles University, Prague, Czech Republic
Abstract
ABSTRACT
Tenofovir diphosphate (PMPApp) is a weak inhibitor of DNA polymerases (pol) α, δ, and ε*, with values for the
K
i
for PMPApp (
PMPApp
K
i
) relative to the
K
m
for dATP (
dATP
K
m
) of 10.2, 10.2, and 15.2, respectively. Its incorporation into DNA was about 1,000-fold less efficient than that of dATP, with
PMPApp
K
m
values 350-, 2,155-, and 187-fold higher than
dATP
K
m
values for pol α, δ, and ε*, respectively.
Publisher
American Society for Microbiology
Subject
Infectious Diseases,Pharmacology (medical),Pharmacology
Reference31 articles.
1. Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxyethyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, (R)-9-(2-phosphonylmethoxypropyl)adenine, and MDL 74,968] in cell cultures and murine sarcoma virus-infected newborn NMRI mice
2. Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine
3. Phase I/II Trial of the Pharmacokinetics, Safety, and Antiretroviral Activity of Tenofovir Disoproxil Fumarate in Human Immunodeficiency Virus-Infected Adults
4. Assessment of Mitochondrial Toxicity in Human Cells Treated with Tenofovir: Comparison with Other Nucleoside Reverse Transcriptase Inhibitors
5. Birkuš, G., I. Votruba, B. Otová, M. Otmar, and A. Holý. 1999. HPMPApp as a substrate toward replicative DNA polymerases α, δ and ε, p. 289-293. In A. Holý and M. Hocek (ed.), Collection symposium series,vol. 2. Institute of Organic Chemistry and Biochemistry, Academy of Sciences of Czech Republic, Prague.
Cited by
37 articles.
订阅此论文施引文献
订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献