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翻譯整理自國考參考書Foye’s 7th   Page. 296 不可逆酵素抑制劑有兩種： 1. Affinity labels（也稱為active site-directed irreversible inhibitors ）2. Mechanism-based irreversible enzyme inactivators.   Affinity Labels 1.      本身為酵素的受質 2.      可以和任何酵素中的親核性基團結合（特別是催化中心部位附近的） 3.      本身為親電子性（常見基團：halo-methyl ketones (X-CH2C=O)、sulfonyl fluorides (SO2F)、nitrogen mustards [(ClCH2CH2)2NH]、diazoketones (COCHN2)） 4.      治療價值低（因為其為非選擇性，因此本性上具毒性） 5.      通常用作生化研究工具（...
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翻譯整理自國考參考書Foye’s 7th   Page. 296 不可逆酵素抑制劑有兩種： 1. Affinity labels（也稱為active site-directed irreversible inhibitors ）2. Mechanism-based irreversible enzyme inactivators.   Affinity Labels 1.      本身為酵素的受質 2.      可以和任何酵素中的親核性基團結合（特別是催化中心部位附近的） 3.      本身為親電子性（常見基團：halo-methyl ketones (X-CH2C=O)、sulfonyl fluorides (SO2F)、nitrogen mustards [(ClCH2CH2)2NH]、diazoketones (COCHN2)） 4.      治療價值低（因為其為非選擇性，因此本性上具毒性） 5.      通常用作生化研究工具（探測催化位及附近的氨基酸種類差異） 6.      經典例子為：TPCK (tosyl-phenylalanyl-chloromethyl-ketone)，serine protease chymotrypsin的不可逆抑制劑 原文： The affinity labels are those chemical entities that are inherently reactive and can target any nucleophilic group in the enzyme, especially those residing in and around the catalytic center of the protein. These agents generally resemble the substrate so that they can bind in the active site of the enzyme. In most examples, these agents also contain an electrophilic group, which includes groups such as halo-methyl ketones (X-CH2C=O, where X = halide), sulfonyl fluorides (SO2F), nitrogen mustards [(ClCH2CH2)2NH], diazoketones (COCHN2), and other such reactive groups, that can “label,” or alkylate, a nucleophilic amino acid group in the enzyme. They generally tend to be indiscriminate in their action and have little therapeutic value, because they are nonselective and, thus, inheren.....觀看完整全文，請先登入