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transition state analogs
相关语句
  过渡态类似物
     The transition state analogs, 2-NH2-galactose and L-ribose were almost the same effects for the mutated enzymes as for the normal enzyme.
     无论是天然酶还是突变酶,底物类似物IPTG是一个强有力的抑制剂,而过渡态类似物2-脱氧-2-氨基-半乳糖和L-核糖只对突变酶有微弱的抑制作用.
短句来源
     The Development of the Carbenium Transition State Analogs
     正碳离子样的过渡态类似物研究进展
短句来源
  相似匹配句对
     MODEL STATE TRANSITION OF PENDULUM
     摆渡问题的状态转移模型
短句来源
     state.
     state.
短句来源
     State and V. T.
     Stace和V.T.
     On the Aromatic Transition State Theory
     芳香过渡态理论及其应用
短句来源
     The Development of the Carbenium Transition State Analogs
     正碳离子样的过渡态类似物研究进展
短句来源
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  transition state analogs
Two recurring observations, that were not expected in theory, have been the binding of inhibitors in ionized forms that are rare in solution, and changes in enzyme configuration that accompany binding of transition state analogs.
      
Sterol Biosynthesis Inhibitors: Potential for Transition State Analogs and Mechanism-Based Inactivators Targeted at Sterol Methy
      
Implications of these calculations for the computer-aided design of transition state analogs for the induction of catalytic antibodies are discussed.
      
This information can be applied to the development of transition state analogs and mechanism-based inhibitors of PurE Class I.
      
This suggests the possibility for abzyme production via the pathway described for antibodies induced by transition state analogs.
      
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Glutamic acid at position of 537 of β-D-galactosidase coded by Lac Z gene was substituted with Aspartic acid, Glutamine and Valine using synthetic oligonucleotide probes. Compared to native enzyme, the kcal values for substrate ONPG were 0. 13%, 0.0006% and 0.0035% for Asp-537, Gln-537 and Val-537 mutated enzymes respectively. The Km values were of the same order of magnitude, either native or mutated enzymes. The substrate analog, IPTG was a strong inhibitor of each of the substituted enzymes, as in the case...

Glutamic acid at position of 537 of β-D-galactosidase coded by Lac Z gene was substituted with Aspartic acid, Glutamine and Valine using synthetic oligonucleotide probes. Compared to native enzyme, the kcal values for substrate ONPG were 0. 13%, 0.0006% and 0.0035% for Asp-537, Gln-537 and Val-537 mutated enzymes respectively. The Km values were of the same order of magnitude, either native or mutated enzymes. The substrate analog, IPTG was a strong inhibitor of each of the substituted enzymes, as in the case of native enzyme. The transition state analogs, 2-NH2-galactose and L-ribose were almost the same effects for the mutated enzymes as for the normal enzyme. The nucleophili, Azide, did not activate the mutated enzymes as in the case of Glu-461 substituted in β-D-galactosidase. The effect of methanol on the mutated enzymes was less than on native enzyme. The order of the thermal stability was native enzyme > Asp-537>Gln-537> Val-537 enzymes. Overall, the evidence strongly supports the suggestion that Glu-537 is an essential residue ofβ-D-galactosidase.

利用人工合成的寡核苷酸探针,将编码大肠杆菌β-D-半乳糖苷酶(EC3.2.1.23)的Lac Z基因中537位Glu密码子GAA分别用GAC(Asp)、CAA(Gln)、GTC(Val)来替代,替代后的突变酶的催化活性显著降低.同天然β-D-半乳糖苷酶相比,作用于ONPG底物时,突变酶的k_(cat)值分别为0.13%(Asp-537)、0.0006%(Gln-537)、0.0035%(Val-537),但它们的K_m值并无明显改变.无论是天然酶还是突变酶,底物类似物IPTG是一个强有力的抑制剂,而过渡态类似物2-脱氧-2-氨基-半乳糖和L-核糖只对突变酶有微弱的抑制作用.活化剂叠氮钠的激活作用小于β-D-半乳糖苷酶的Glu-461突变酶.催化甲醇成酯反应的能力小于天然酶.突变酶对热更不稳定.以上结果表明Glu-537残基是该酶催化反应的必需基团.

An important feature in the enzyme catalyzed reaction is that an enzyme recognizes and binds more tightly to the transition state than to the ground state of the substrate product interconversion.The transition state analog must be a potent inhibitor of the enzyme.The recent development of the carbenium transition state analogs as the enzymatic inhibitors which are designed by the transition state theory of enzyme catalyzed reactions is reviewed.Four types of enzymatic inhibitors including...

An important feature in the enzyme catalyzed reaction is that an enzyme recognizes and binds more tightly to the transition state than to the ground state of the substrate product interconversion.The transition state analog must be a potent inhibitor of the enzyme.The recent development of the carbenium transition state analogs as the enzymatic inhibitors which are designed by the transition state theory of enzyme catalyzed reactions is reviewed.Four types of enzymatic inhibitors including the transition state analogs of isoprenoid pyrophosphate,sialyltransferase,KDO8P and UGT are introduced.

综述了应用酶催化过渡态理论设计的几类正碳离子样的过渡态类似物作为酶的抑制剂的研究进展。其中包括类异戊二烯的正离子过渡态类似物,唾液酸转移酶的过渡态类似物,3-脱氧-D-甘露糖-2-辛酮糖酸酯-8-磷酸酯(KDO8P)合成酶的过渡态类似物,尿苷二磷酸酯葡糖醛酸基转移酶(UGT)的过渡态类似物。

 
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