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A distamycin analog selectively blocks chemokine receptor function and HIV-1 fusion

  1. Author:
    Turpin, J. A.
    Rice, W. G.
    Oppenheim, J. J.
    Hollingshead, M. G.
    Covey, J. M.
    Howard, O. M.
    1. Year of Conference: 1998
  2. Conference Name: HIV Pathogenesis and Treatment Conference
    1. Pages: 57 (abstract no. 2042)
  4. Type of Work: Meeting Abstract
  1. Abstract:

    We have identified a distamycin analog, 2,2'[4,4'[[aminocarbonyl]amino] bis[N,4'-di[pyrrole-2-carboxamide-1,1'-dimethyl] ]-6,8 napthylenedisulfonic acid]hexasodium salt(NSC 651016) which inhibits HIV-1 replication by interfering with the interaction of HIV-1 with chemokine co-receptors. NSC 651016 inhibited HIV-1 fusion, but not virus attachment. Subsequently, it was found to inhibit virus replication in 293 cells transiently co-transfected with CD4 and CCR5 or CXCR4. Furthermore, it selectively inhibited chemokine binding to CCR5, CCR3 and CXCR4, but not to CXCR2 or CCR2b, and blocked Ca flux and chemotaxis by human blood monocytes in response to specific chemokine ligands. A closely related analog and the monomeric form of NSC 651016 were inactive, and NSC 651016 failed to effect FMLP induced chemotaxis or Ca flux. NSC 651016 also inhibited HIV-1 replication in an in vivo mouse model with low organ toxicity and 100% subcutaneous bioavailability. Thus, NSC 651016 mediates inhibition of HIV-1 replication by selectively interfering with chemokine co-receptors.

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