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Effect of HIV integrase inhibitors on the RAG1/2 recombinase

  1. Author:
    Melek, M.
    Jones, J. M.
    O'Dea, M. H.
    Pais, G.
    Burke, T. R.
    Pommier, Y.
    Neamati, N.
    Gellert, M.

  2. Author Address

    NIDDKD, Mol Biol Lab, NIH, Bldg 5, Room 241, Bethesda, MD 20892 USA. NIDDKD, Mol Biol Lab, NIH, Bethesda, MD 20892 USA. NCI, Canc Res Ctr, Med Chem Lab, Frederick, MD 21702 USA. NCI, Mol Pharmacol Lab, Div Basic Sci, Bethesda, MD 20892 USA. Gellert M NIDDKD, Mol Biol Lab, NIH, Bldg 5, Room 241, Bethesda, MD 20892 USA.
    1. Year: 2002
  2. Journal: Proceedings of the National Academy of Sciences of the United States of America
    1. 99
    2. 1
    3. Pages: 134-137
  4. Type of Article: Article
  1. Abstract:

    Assembly of functional Ig and T cell receptor genes by V(D)J recombination depends on site-specific cleavage of chromosomal DNA by the RAG1/2 recombinase. As RAG1/2 action has mechanistic similarities to DNA transposases and integrases such as HIV-1 integrase, we sought to determine how integrase inhibitors of the diketo acid type would affect the various activities of RAG1/2. Both of the inhibitors we tested interfered with DNA cleavage and disintegration activities of RAG1/2, apparently by disrupting interaction with the DNA motifs bound specifically by the recombinase. The inhibitors did not ablate RAG1/2's transposition activity or capture of nonspecific transpositional target DNA, suggesting this DNA occupies a site on the recombinase different from that used for specific binding. These results further underscore the similarities between RAG1/2 and integrase and suggest that certain integrase inhibitors may have the potential to interfere with aspects of B and T cell development.

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