鉴定克氏锥虫复制的小分子抑制剂。
Identification of small-molecule inhibitors of Trypansoma cruzi replication.
机构信息
Chemical Biology Platform and Probe Development Center, Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA.
出版信息
Bioorg Med Chem Lett. 2011 Dec 1;21(23):7197-200. doi: 10.1016/j.bmcl.2011.09.057. Epub 2011 Sep 29.
We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds were identified that displayed nanomolar inhibition of T. cruzi and an absence of activity against host cells at the highest tested dose. These compounds have been registered with NIH Molecular Libraries Program (probes ML157 and ML158).
我们报告了高通量小分子筛选的结果，以鉴定新型无毒的 Trypansoma cruzi 抑制剂，作为治疗恰加斯病急性和慢性阶段的潜在治疗起点。鉴定出两种化合物，它们对 T. cruzi 的抑制作用达到纳摩尔级，并且在最高测试剂量下对宿主细胞没有活性。这些化合物已在 NIH 分子库计划（探针 ML157 和 ML158）中注册。
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