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Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds
O M Howard1, H F Dong, J J Oppenheim
1Laboratory of Molecular Immunoregulation, National Cancer Istitute-Frederick Cancer Research and Development Center, MD 21702, USA. howardz@mail.ncifcrf.gov
Bioorganic & Medicinal Chemistry Letters
|January 5, 2001
Abstract:
The anti-HIV agent cosalane and several of its analogues inhibited RANTES-induced migration of human monocytes, but they did not inhibit migration induced by MIP1alpha or MIP1beta. RANTES-induced migration of single receptor CCRI-HEK transfectants was also inhibited by the cosalanes. Acetylation of the reactive amino groups of RANTES abrogated the inhibitory activity of cosalane. The data suggest that cosalane and its structural analogues may interfere with the RANTES/CCR1 interaction by binding to RANTES.