New class of competitive inhibitor of bacterial histidine kinases
New class of competitive inhibitor of bacterial histidine kinases
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DOI：
10.1128/jb.187.23.8196-8200.2005
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发表时间：
2005-12-01
影响因子：
3.2
通讯作者：
Winkler, ME
中科院分区：
文献类型：
--
作者：
Gilmour, R;Foster, JE;Winkler, ME
细菌组氨酸激酶已被提议作为发现新抗生素的靶点，但很少有细菌组氨酸激酶的特异性抑制剂的报道。我们在这里报告了一种新的噻吩并吡啶（TEP）化合物，抑制细菌组氨酸激酶竞争性相对于ATP，但不抑制哺乳动物丝氨酸/苏氨酸激酶。尽管TEP分配到细胞膜中并且不抑制细菌或哺乳动物细胞的生长，但它可以作为一类具有抗菌活性的新型组氨酸激酶抑制剂的起始化合物。
Bacterial histidine kinases have been proposed as targets for the discovery of new antibiotics, yet few specific inhibitors of bacterial histidine kinases have been reported. We report here a novel thienopyridine (TEP) compound that inhibits bacterial histidine kinases competitively with respect to ATP but does not comparably inhibit mammalian serine/threonine kinases. Although it partitions into membranes and does not inhibit the growth of bacterial or mammalian cells, TEP could serve as a starting compound for a new class of histidine kinase inhibitors with antibacterial activity.