一种有机金属谷胱甘肽转移酶抑制剂的合理设计。
Rational design of an organometallic glutathione transferase inhibitor.
作者信息
Ang Wee Han, Parker Lorien J, De Luca Anastasia, Juillerat-Jeanneret Lucienne, Morton Craig J, Lo Bello Mario, Parker Michael W, Dyson Paul J
机构信息
Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne, 1015 Lausanne, Switzerland.
出版信息
Angew Chem Int Ed Engl. 2009;48(21):3854-7. doi: 10.1002/anie.200900185.
Double trouble: A hybrid organic-inorganic (organometallic) inhibitor was designed to target glutathione transferases. The metal center is used to direct protein binding, while the organic moiety acts as the active-site inhibitor (see picture). The mechanism of inhibition was studied using a range of biophysical and biochemical methods.
双重难题
设计了一种有机-无机（有机金属）混合抑制剂来靶向谷胱甘肽转移酶。金属中心用于引导蛋白质结合，而有机部分作为活性位点抑制剂（见图）。使用一系列生物物理和生化方法研究了抑制机制。
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