新型细菌DNA回旋酶抑制剂GR122222X的作用模式
Mode of action of GR122222X, a novel inhibitor of bacterial DNA gyrase.
作者信息
Oram M, Dosanjh B, Gormley N A, Smith C V, Fisher L M, Maxwell A, Duncan K
机构信息
Department of Cellular and Molecular Sciences, University of London, United Kingdom.
出版信息
Antimicrob Agents Chemother. 1996 Feb;40(2):473-6. doi: 10.1128/AAC.40.2.473.
Abstract
GR122222X is a potent inhibitor of the supercoiling reaction of bacterial DNA gyrase. We show that this compound binds stoichiometrically to inactivate the ATPase activity of a 43-kDa N-terminal fragment of the B subunit and competitively inhibits the binding of a radiolabelled coumarin drug to N-terminal fragments of GyrB. These and other data suggest that GR122222X has a mode of action similar, but not identical, to that of coumarin antibiotics.
摘要
GR122222X是细菌DNA促旋酶超螺旋反应的强效抑制剂。我们发现该化合物以化学计量方式结合，使B亚基43 kDa N端片段的ATP酶活性失活，并竞争性抑制放射性标记香豆素药物与GyrB N端片段的结合。这些及其他数据表明，GR122222X的作用模式与香豆素类抗生素相似，但并不完全相同。
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