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Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA.

Publication ,  Journal Article
Weinberg, JB; Shugars, DC; Sherman, PA; Sauls, DL; Fyfe, JA
Published in: Biochem Biophys Res Commun
May 19, 1998

Our prior studies showed that certain cobalamins inhibit productive HIV-1 infection of primary cultures of blood lymphocytes and monocytes. We demonstrate here that this antiviral activity may be mediated by an inhibition of HIV-1 integrase, an enzyme required for productive infection. Purified recombinant HIV-1 integrase activity was inhibited in vitro by hydroxocobalamin (OH-Cbl), methylcobalamin (Me-Cbl), adenosylcobalamin (Ado-Cbl), and dicyanocobinamide (CN2-Cbi) with IC50 values of approximately 17, 17, 17, and 4 microM, respectively. The agents inhibited HIV-1 infection of cultured monocytes (IC50 values for OH-Cbl, Me-Cbl, Ado-Cbl, and CN2-Cbi of 6, 7, 4, and 1 microM, respectively) and of cultured lymphocytes (IC50 values of 60, 50, 60, and 11 microM, respectively). Experiments using cultured monocytes or lymphocytes demonstrated that OH-Cbl inhibited integration of HIV-1 DNA into cellular DNA. Thus, cobalamins and cobinamides represent novel inhibitors of HIV-1 integrase. These or related agents may be useful as anti-viral treatments that target HIV-1 integrase.

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Published In

Biochem Biophys Res Commun

DOI

ISSN

0006-291X

Publication Date

May 19, 1998

Volume

246

Issue

2

Start / End Page

393 / 397

Location

United States

Related Subject Headings

  • Vitamin B 12
  • Virus Integration
  • Polymerase Chain Reaction
  • Monocytes
  • Lymphocytes
  • In Vitro Techniques
  • Hydroxocobalamin
  • Humans
  • HIV-1
  • HIV Integrase Inhibitors
 

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Weinberg, J. B., Shugars, D. C., Sherman, P. A., Sauls, D. L., & Fyfe, J. A. (1998). Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA. Biochem Biophys Res Commun, 246(2), 393–397. https://doi.org/10.1006/bbrc.1998.8629
Weinberg, J. B., D. C. Shugars, P. A. Sherman, D. L. Sauls, and J. A. Fyfe. “Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA.Biochem Biophys Res Commun 246, no. 2 (May 19, 1998): 393–97. https://doi.org/10.1006/bbrc.1998.8629.
Weinberg JB, Shugars DC, Sherman PA, Sauls DL, Fyfe JA. Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA. Biochem Biophys Res Commun. 1998 May 19;246(2):393–7.
Weinberg, J. B., et al. “Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA.Biochem Biophys Res Commun, vol. 246, no. 2, May 1998, pp. 393–97. Pubmed, doi:10.1006/bbrc.1998.8629.
Weinberg JB, Shugars DC, Sherman PA, Sauls DL, Fyfe JA. Cobalamin inhibition of HIV-1 integrase and integration of HIV-1 DNA into cellular DNA. Biochem Biophys Res Commun. 1998 May 19;246(2):393–397.
Journal cover image

Published In

Biochem Biophys Res Commun

DOI

ISSN

0006-291X

Publication Date

May 19, 1998

Volume

246

Issue

2

Start / End Page

393 / 397

Location

United States

Related Subject Headings

  • Vitamin B 12
  • Virus Integration
  • Polymerase Chain Reaction
  • Monocytes
  • Lymphocytes
  • In Vitro Techniques
  • Hydroxocobalamin
  • Humans
  • HIV-1
  • HIV Integrase Inhibitors