Improved photocontrol of alpha-chymotrypsin activity: Peptidomimetic trifluoromethylketone photoswitch enzyme inhibitors

Pearson D; Alexander N; Abell AD

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Improved photocontrol of alpha-chymotrypsin activity: Peptidomimetic trifluoromethylketone photoswitch enzyme inhibitors

机译：改进的α-胰凝乳蛋白酶活性的光控制：拟肽三氟甲基酮光开关酶抑制剂

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A series of peptidomimetic trifluoromethylketones containing the photoisomerisable azobenzene group have been synthesised, photoisomerised and as-sayed against the serine protease alpha-chymotrypsin. All are inhibitors of the enzyme and exhibit up to a fivefold increase in activity on UV irradiation. Visible irradiation returns activity to close to that of the original sample. These results suggest the trifluoromethylketone group to be the best electrophilic enzyme binding group for use in photoswitch inhibitors of alpha-chymotrypsin.

机译：已经合成，光异构化并针对丝氨酸蛋白酶α-胰凝乳蛋白酶测定了一系列含有可光异构的偶氮苯基的拟肽三氟甲基酮。所有这些都是酶的抑制剂，并且在紫外线照射下的活性最多增加五倍。可见辐射使活性恢复到接近原始样品的活性。这些结果表明，三氟甲基酮基团是用于α-胰凝乳蛋白酶的光开关抑制剂的最佳亲电子酶结合基团。

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《Chemistry: A European journal》 |2008年第24期|共8页
作者
Pearson D; Alexander N; Abell AD;
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正文语种 eng
中图分类化学;
关键词
azo compounds; enzymes; molecular devices; peptidomimetics; photochromism; PEPTIDYL FLUOROMETHYL KETONES; PHOTOBIOLOGICAL SWITCHES; SERINE PROTEASES; BINDING; PHOTOREGULATION; OXIDATION; ESTERS; H2O2;

机译：偶氮化合物;酶;分子器件;拟肽;光致变色;肽基氟甲基酮;光生物开关;丝氨酸蛋白酶;键合;光调节;氧化;酯;H2O2;

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机译：改进的α-胰凝乳蛋白酶活性的光控制：拟肽三氟甲基酮光开关酶抑制剂
2. Oxymatrine attenuated hypoxic-ischemic brain damage in neonatal rats via improving antioxidant enzyme activities and inhibiting cell death [J] . Zhao Peng, Zhou Ru, Li Hai-Ning, Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry . 2015,第Null期

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Improved photocontrol of alpha-chymotrypsin activity: Peptidomimetic trifluoromethylketone photoswitch enzyme inhibitors

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