Department of Microbial Natural Products, Helmholtz-Institute for Pharmaceutical Research Saarland HIPS, Helmholtz Centre for Infection Research HZI and Department of Pharmaceutical Biotechnology, Saarland University, Campus C2 3, 66123 Saarbrücken, Germany.
Chembiochem. 2013 Jul 8;14(10):1194-7. doi: 10.1002/cbic.201300208. Epub 2013 Jun 6.
Releasing the cytopath: We have identified an N-myristoyl-D-asparagine (1) as the free N-terminal prodrug scaffold in cytopathogenic Escherichia coli strains expressing the colibactin gene cluster. Colibactin is released in vivo upon cleavage of precolibactin. We provide for the first time in vivo evidence of the prodrug-like release mechanism of colibactin.
我们已经确定了 N-豆蔻酰-D-天冬酰胺（1）作为表达肠毒素基因簇的细胞致病性大肠杆菌菌株中游离的 N 端前药支架。在预肠毒素切割时，肠毒素在体内释放。我们首次提供了肠毒素前药样释放机制的体内证据。
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