L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro anti-HIV-1 effect of Zidovudine plus a protease inhibitor (AG1350).
L-chicoric acid, an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase, improves on the in vitro anti-HIV-1 effect of Zidovudine plus a protease inhibitor (AG1350).
复制标题
L-菊苣酸是 1 型人类免疫缺陷病毒 (HIV-1) 整合酶的抑制剂，可改善齐多夫定加蛋白酶抑制剂 (AG1350) 的体外抗 HIV-1 效果。
DOI：
10.1016/s0166-3542(98)00037-0
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发表时间：
1998
影响因子：
7.6
通讯作者：
RobinsonJr,WE
中科院分区：
文献类型：
--
作者：
RobinsonJr,WE
Combinations of anti-human immunodeficiency virus (HIV) drugs, including reverse transcriptase inhibitors and protease inhibitors, have proven immensely potent in the therapy of acquired immune deficiency syndrome (AIDS). To determine whether HIV integrase is a suitable target for combination therapy, the ability of an HIV integrase inhibitor, l-chicoric acid, to work in combination with a protease inhibitor and Zidovudine was tested in vitro. The addition of l-chicoric acid to either Zidovudine or protease inhibitor improved upon the observed anti-HIV activity of either compound alone. When all three drugs were combined, the anti-HIV activity was substantially better than either of the three compounds alone or any combination of two inhibitors. Doses of both Zidovudine and protease inhibitor could be reduced by more than 33% for an equivalent anti-HIV effect if l-chicoric acid was added. The improved anti-HIV activity was observed with a tissue culture adapted strain of HIV (HIVLAI) and with limited passage clinical isolates of HIV (HIVR19and HIVR45). These data demonstrate that a first generation HIV integrase inhibitor, l-chicoric acid, is at least additive in combination with existing multi-drug regimens and suggest that HIV integrase will be an excellent target for combination therapy of HIV infection.
