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Antimicrobial Agents and Chemotherapy, May 2002, p. 1610-1613, Vol. 46, No. 5
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.5.1610-1613.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Tenofovir Diphosphate Is a Poor Substrate and a Weak Inhibitor of Rat DNA Polymerases {alpha}, {delta}, and {varepsilon}*

Gabriel Birkus,1* Miroslav Hájek,1 Pavel Kramata,1 Ivan Votruba,1 Antonín Holy,1 and Berta Otová2

Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic,,1 Institute of Biology and Medical Genetics, 1st Faculty of Medicine and General Teaching Hospital, Charles University, Prague, Czech Republic2

Received 30 August 2001/ Returned for modification 4 December 2001/ Accepted 4 February 2002

Tenofovir diphosphate (PMPApp) is a weak inhibitor of DNA polymerases (pol) {alpha}, {delta}, and {varepsilon}*, with values for the Ki for PMPApp (PMPAppKi) relative to the Km for dATP (dATPKm) 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 PMPAppKm values 350-, 2,155-, and 187-fold higher than dATPKm values for pol {alpha}, {delta}, and {varepsilon}*, respectively.

* Corresponding author. Mailing address: Gilead Sciences, 333 Lakeside Dr., Foster City, CA 94404. Phone: (650) 522-5957. Fax: (650) 522-5890. E-mail: Gabriel_Birkus{at}gilead.com.

Antimicrobial Agents and Chemotherapy, May 2002, p. 1610-1613, Vol. 46, No. 5
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.5.1610-1613.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Boffito, M., Pozniak, A., Kearney, B. P., Higgs, C., Mathias, A., Zhong, L., Shah, J. (2005). Lack of Pharmacokinetic Drug Interaction between Tenofovir Disoproxil Fumarate and Nelfinavir Mesylate. Antimicrob. Agents Chemother. 49: 4386-4389 [Abstract] [Full Text]  
  • De Clercq, E. (2003). Clinical Potential of the Acyclic Nucleoside Phosphonates Cidofovir, Adefovir, and Tenofovir in Treatment of DNA Virus and Retrovirus Infections. Clin. Microbiol. Rev. 16: 569-596 [Abstract] [Full Text]  


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