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Identification of potential HIV-1 integrase (IN) inhibitors by co-localization of antiviral activity with integrase mediated events in the retroviral replication cycle

  1. Author:
    Rice, W. G.
    Schaeffer, C. A.
    Bu, M.
    Williamson, K.
    Turpin, J. A.
    1. Year of Conference: 1998
  2. Conference Name: HIV Pathogenesis and Treatment Conference
    1. Pages: 55 (abstract no. 2036)
  4. Type of Work: Meeting Abstract
  1. Abstract:

    Even though triple combination antiviral cocktails have shown great promise in the treatment of AIDS, we are still faced with developing new antivirals to address persistent low level replication of HIV. IN has been identified as a choice target for new antivirals, but its full potential has yet to be realized due to the inability to adequately relate the oligo based 3' processing and strand transfer assay to antiviral activity. As part of the NCI drug screening initiative we determined cellular and mechanistic antiviral action profiles on over 400 compounds with moderate anti-HIV-1 activity in an XTT cyto-protection assay. Compounds were assessed for effects on reverse transcriptase, virus attachment, IN, protease, reactivity with the NCp7 Zn fingers, and inhibition of replication in latently infected U1 cells. Using these activity profiles compounds were selected for further evaluation ultimately leading to 8 lead compounds which inhibit IN, exhibit moderate antiviral activity but fail to affect any other viral target. Thus, we have identified several promising lead compounds that are temporally associated with integrase inhibition within cells.

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