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wzg389960金虫 (小有名气)
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GSTs are divided into two groups: the membrane-bound microsomal and the cytosolic GSTs. Microsomal GSTs exist in homo- and hetero-trimerized forms with a single active site and function in the endogenous metabolism of leuco-trienes and prostaglandins [8]. In humans, cytosolic GSTs exist in the form of various dimerized isoenzyme classes: (A), μ (M), , (P), (T), (Z) and classes[8,13]. Their existence in different forms has provided broadsubstrate specificities promoting detoxification of many toxic substances. Recently, the X-ray crystal structure of GST of the malaria-causing parasite, Plasmodium falciparum, was elucidated [14]. The isoenzymes of GST are related in their aminoacid constituents and a little in their conformation except at specific regions, two of which are needed for activity. This distinguishing uniqueness is attributed to the catalytic hydrophobic site (H-site) and a glutathione-binding site (G-site), which offer diversity in specificities of the different isoenzymes for different substrates. In addition to their xenobiotic detoxification roles, human and parasitic GSTs have been implicated as lead actors in cellular drug resistances, which is a major factor in the failure of chemotherapy [15]. Electrophilic alkylating anticancer and antiparasitic drugs have been reported to be either substrates or ligands for the different GST isoenzymes [16], and this forms the basis of cellular drug resistances. |
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wangyuan0929
金虫 (小有名气)
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RXMCDM: 金币+1, 多谢应助！ 2014-03-14 00:56:23
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GSTs are divided into two groups: the membrane-bound microsomal and the cytosolic GSTs. GST被分为两组：膜结合的微粒体GST和胞浆GST。 Microsomal GSTs exist in homo- and hetero-trimerized forms with a single active site and function in the endogenous metabolism of leucotrienes and prostaglandins [8]. 微粒体GST以同三聚体或异三聚体形式存在，它只有一个活性中心，并在白细胞三烯和前列腺素的胞内代谢中起作用。 In humans, cytosolic GSTs exist in the form of various dimerized isoenzyme classes: (A), μ (M), , (P), (T), (Z) and classes[8,13]. 在人类中，胞浆GST以多种二聚体同工酶形式存在：（略）。 Their existence in different forms has provided broad substrate specificities promoting detoxification of many toxic substances. 不同形式的胞浆GST的存在为其提供了宽泛的特异性底物范围，这促进了许多种有毒底物的解毒作用。 Recently, the X-ray crystal structure of GST of the malaria-causing parasite, Plasmodium falciparum, was elucidated [14]. 最近导致疟疾的寄生虫——恶性疟原虫的GST的X射线晶体结构得到了阐明。 The isoenzymes of GST are related in their aminoacid constituents and a little in their conformation except at specific regions, two of which are needed for activity. GST的同工酶在其氨基酸组成上相互关联，除了在特定区域之外，其构象也相互关联，其中两个特定区域对于其活性是必需的。 This distinguishing uniqueness is attributed to the catalytic hydrophobic site (H-site) and a glutathione-binding site (G-site), which offer diversity in specificities of the different isoenzymes for different substrates. 这种造成区别的独特性属于催化性的疏水位点（H位点）和一个谷胱甘肽结合位点（G位点），它们为不同同工酶对不同底物的特异性提供了多样性。 In addition to their xenobiotic detoxification roles, human and parasitic GSTs have been implicated as lead actors in cellular drug resistances, which is a major factor in the failure of chemotherapy [15]. 除了对异生物质的解读作用之外，人类和寄生虫的GST也是细胞的药物抗性的首要作用物质，而这正是化学疗法失效的主要因素。 Electrophilic alkylating anticancer and antiparasitic drugs have been reported to be either substrates or ligands for the different GST isoenzymes [16], and this forms the basis of cellular drug resistances. 据报道，亲电子烷化抗癌和抗寄生虫药物可以充当不同GST同工酶的底物或配体，这一现象构成了细胞药物抗性的基础。 |
2楼2014-03-13 21:19:15