为构建高活性智能人工酶，选择谷胱甘肽硫转移酶作为人工酶骨架，将其124号位赖氨酸突变为半胱氨酸，通过点击化学反应，在pH = 6.0时将基于葫芦［6］脲并具有pH响应性的超分子开关精确修饰于人工酶骨架的催化口袋处，具有较大体积和较强刚性的开关分子可以有效阻碍底物进入催化口袋之中，因此仅能展现3%的催化活性，从而实现人工酶活性的“关闭”；将体系pH调控至7.5时，超分子开关发生解离导致葫芦［6］脲分子从催化口袋处脱离，底物进入催化口袋的过程不再受到阻碍，因此能够展现90 %以上的催化活性，从而实现人工酶活性的“开启”。对体系pH在6.0 ~ 7.5进行反复调控，经过5个循环之后对人工酶活性开启和关闭的调控依然有效。因此，利用超分子开关的复合与解离，成功实现了对谷胱甘肽硫转移酶活性可逆“关闭”与“开启”的调控，进而构建了高活性的pH响应性智能人工酶。

In order to construct high activity smart artificial enzyme, schistosoma japonicum glutathione sulfotransferase (sjGST) was selected as the artificial enzyme skeleton and lysine at position of 124 was mutated to cysteine. pH-responsive supramolecular switch based on cucurbit[6] uril was modified exactly to the catalytic pocket of the artificial enzyme skeleton by a click chemistry reaction at pH = 6.0. The large and rigid switch molecule could effectively prevent the substrate from entering the catalytic pocket. Activity of artificial enzyme was "closed" as sjGST show only 3% catalytic activity at this time. The supramolecular switch was dissociated at pH = 7.5 resulting in cucurbit[6] uril to be away from catalytic pocket. The substrate could enter the catalytic pocket freely at this time. Activity of artificial enzyme was "open" as sjGST show more than 90% catalytic activity at this time. The reversible close and open of the artificial enzyme activity could be still achieved after 5 cycles of repeated regulation of the system pH between 6.0 and 7.5. As a result, the reversible close and open regulation of sjGST catalytic activity was successfully achieved utilizing the association and dissociation of supramolecular switch. By this way a high activity pH-responsive smart artificial enzyme was successful constructed.