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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Walkmycin B targets WalK (YycG), a histidine kinase essential for bacterial cell growth.
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Walkmycin B targets WalK (YycG), a histidine kinase essential for bacterial cell growth.

机译：Walkmycin B靶向WalK（YycG），这是细菌细胞生长必不可少的组氨酸激酶。

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摘要

The WalK (a histidine kinase)/WalR (a response regulator, aka YycG/YycF) two-component system is indispensable in the signal transduction pathway for the cell-wall metabolism of Bacillus subtilis and Staphylococcus aureus. The inhibitors directed against WalK would be expected to have a bactericidal effect. After we screened 1368 culture broths of Streptomyces sp. by a differential growth assay, walkmycin A, B and C, which were produced by strain MK632-100F11, were purified using silica-gel column chromatography and HPLC. In this paper, the chemical structure of the major product (walkmycin B) was determined to be di-anthracenone (C(44)H(44)Cl(2)O(14)), which was very similar to BE40665A. MICs of walkmycin B against B. subtilis and S. aureus were 0.39 and 0.20 microg ml(-1), and IC(50) measurements against WalK were 1.6 and 5.7 microM, respectively. To clarify the affinity between WalK and walkmycin B, surface plasmon resonance was measured to obtain the equilibrium dissociation constant, K(D1), of 7.63 microM at the higher affinity site of B. subtilis WalK. These results suggest that walkmycin B inhibits WalK autophosphorylation by binding to the WalK cytoplasmic domain.
机译：枯草芽孢杆菌和金黄色葡萄球菌的细胞壁代谢的信号转导途径中，WalK（组氨酸激酶）/ WalR（响应调节剂，也称为YycG / YycF）两组分系统必不可少。预期针对WalK的抑制剂具有杀菌作用。在我们筛选了1368种链霉菌的培养液后。通过差异生长测定法，使用硅胶柱色谱法和HPLC纯化由菌株MK632-100F11产生的Walkmycin A，B和C。在本文中，主要产品（Walkmycin B）的化学结构被确定为双蒽酮（C（44）H（44）Cl（2）O（14）），与BE40665A非常相似。沃克霉素B对枯草芽孢杆菌和金黄色葡萄球菌的MIC分别为0.39和0.20 microg ml（-1），而针对WalK的IC（50）测量值分别为1.6和5.7 microM。为了阐明WalK和Walkmycin B之间的亲和力，测量了表面等离振子共振，以在枯草芽孢杆菌WalK的较高亲和力位置获得7.63 microM的平衡解离常数K（D1）。这些结果表明，Walkmycin B通过与WalK胞质域结合而抑制WalK自磷酸化。

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