De Clercq E
Rega Institute for Medical Research, Department of Microbiology and Immunology, Katholieke Universiteit, Leuven, Belgium.
Mol Pharmacol. 2000 May;57(5):833-9.
The bicyclams represent a new entity of low-molecular weight molecules that inhibit human immunodeficiency virus (HIV) infection through a specific blockade of CXCR4 (fusin), the receptor for the CXC chemokine SDF-1 (soluble-derived factor), which is also used as coreceptor by T-lymphotropic HIV strains to enter their target cells. The bicyclam AMD3100 or 1,1'-[1,4-phenylenebis(methylene)]-bis-1,4, 8,11-tetraazacyclotetradecane octahydrochloride dihydrate, is able to block the CXCR4 receptor and to inhibit HIV replication at nanomolar concentrations while not being toxic to the host cells at 100,000-fold higher concentrations. It is the most specific and most potent CXCR4 antagonist that has been described to date.
双环胺类化合物代表了一类低分子量分子的新实体，它们通过特异性阻断CXCR4（融合素）来抑制人类免疫缺陷病毒（HIV）感染，CXCR4是CXC趋化因子SDF-1（可溶性衍生因子）的受体，嗜T淋巴细胞HIV毒株也将其用作共受体以进入靶细胞。双环胺AMD3100或1,1'-[1,4-亚苯基双（亚甲基）]-双-1,4,8,11-四氮杂环十四烷八盐酸盐二水合物，能够阻断CXCR4受体，并在纳摩尔浓度下抑制HIV复制，而在浓度高出100000倍时对宿主细胞无毒。它是迄今为止所描述的最具特异性和最强效的CXCR4拮抗剂。
