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wzg389960

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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

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RXMCDM: 金幣+1, 多謝應(yīng)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被分為兩組：膜結(jié)合的微粒體GST和胞漿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].
微粒體GST以同三聚體或異三聚體形式存在，它只有一個活性中心，并在白細(xì)胞三烯和前列腺素的胞內(nèi)代謝中起作用。
In humans, cytosolic GSTs exist in the form of various dimerized isoenzyme classes: (A), μ (M), , (P), (T), (Z) and classes[8,13].
在人類中，胞漿GST以多種二聚體同工酶形式存在：（略）。
Their existence in different forms has provided broad substrate specificities promoting detoxification of many toxic substances.
不同形式的胞漿GST的存在為其提供了寬泛的特異性底物范圍，這促進了許多種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].
最近導(dǎo)致瘧疾的寄生蟲——惡性瘧原蟲的GST的X射線晶體結(jié)構(gòu)得到了闡明。
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組成上相互關(guān)聯(lián)，除了在特定區(qū)域之外，其構(gòu)象也相互關(guān)聯(lián)，其中兩個特定區(qū)域?qū)τ谄浠钚允潜匦璧摹?br /> 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.
這種造成區(qū)別的獨特性屬于催化性的疏水位點（H位點）和一個谷胱甘肽結(jié)合位點（G位點），它們?yōu)椴煌っ笇Σ煌孜锏奶禺愋蕴峁┝硕鄻有浴?br /> 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].
除了對異生物質(zhì)的解讀作用之外，人類和寄生蟲的GST也是細(xì)胞的藥物抗性的首要作用物質(zhì)，而這正是化學(xué)療法失效的主要因素。
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.
據(jù)報道，親電子烷化抗癌和抗寄生蟲藥物可以充當(dāng)不同GST同工酶的底物或配體，這一現(xiàn)象構(gòu)成了細(xì)胞藥物抗性的基礎(chǔ)。

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