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PNAS:发光杆菌代谢物有望成为新型抗癌药物

来源:生物谷 2012-12-21 23:10

2012年12月21日讯 /生物谷BIOON/--蛋白酶体能够将蛋白质分解成氨基酸,是细胞维持自身物质平衡的一类重要细胞器。癌细胞表达大量蛋白质,其蛋白酶体负责将多余的蛋白质分解。如果将蛋白酶体阻断,癌细胞大量的垃圾不能被分解,癌细胞会被这些垃圾毒死。

Michael Groll领导的研究团队依照这个思路,大量的筛选能够抑制蛋白酶体的物质。发光杆菌能够产生一类毒素杀死金龟子。研究人员成功的用生化分离的方法鉴定出毒素有两类相似的物质组成,分别是cepafungin I和glidobactin A。已经报道glidobactin A 是一类蛋白酶体抑制剂,由于两类物质结构相似,研究人员发现cepafungin I 同样具有抑制蛋白酶体的功能。

Michael Groll 说,大自然已经进化出了天然的蛋白酶体抑制剂,它们在植物昆虫甚至人类中都有效果,如果利用这类天然物质,将大大提高制药产业的发展。(生物谷Bioon.com)

One-shot NMR analysis of microbial secretions identifies highly potent proteasome inhibitor

Martin L. Stein, Philipp Beck, Markus Kaiser, Robert Dudler, Christian F. W. Becker and Michael Groll

Natural products represent valuable lead structures for drug discovery. However, for most bioactive compounds no cellular target is yet identified and many substances predicted from genome analysis are inaccessible due to their life stage-dependent biosynthesis, which is not reflected in common isolation procedures. In response to these issues, an NMR-based and target-directed protease assay for inhibitor detection of the proteasome was developed. The methodology is suitable for one-shot identification of inhibitors in conglomerates and crude culture broths. The technique was applied for analysis of the different life stages of the bacterium Photorhabdus luminescens, which resulted in the isolation and characterization of cepafungin I (CepI), the strongest proteasome inhibitor described to date. Its biosynthesis is strictly regulated and solely induced by the specific environmental conditions determined by our methodology. The transferability of the developed technique to other drug targets may disclose an abundance of novel compounds applicable for drug development.

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