考沙兰及相关化合物对RANTES/CCR1介导的趋化作用的抑制

Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.

作者信息

Howard O M, Dong H F, Oppenheim J J, Insaf S, Santhosh K C, Paul G, Cushman M

机构信息

Laboratory of Molecular Immunoregulation, National Cancer Istitute-Frederick Cancer Research and Development Center, MD 21702, USA.

出版信息

Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62. doi: 10.1016/s0960-894x(00)00601-6.

DOI:10.1016/s0960-894x(00)00601-6

PMID:11140734

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.

摘要

抗HIV药物科萨烷及其几种类似物可抑制RANTES诱导的人单核细胞迁移，但它们不抑制MIP1α或MIP1β诱导的迁移。科萨烷也可抑制RANTES诱导的单受体CCRI-HEK转染细胞的迁移。RANTES反应性氨基的乙酰化消除了科萨烷的抑制活性。数据表明，科萨烷及其结构类似物可能通过与RANTES结合来干扰RANTES/CCR1相互作用。