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inhibitor
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  相似匹配句对
     Ribonuclease Inhibitor
     核糖核酸酶抑制因子
短句来源
     acetylcholinesterase inhibitor
     乙酰胆碱酯酶抑制药
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  inhibitor
We designed an isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections.
      
Since amlodipine besylate is a very potent inhibitor of both cholinesterases, amlodipine besylate may, like donepezil, be useful in Alzheimer's disease treatment.
      
Efavirenz is a trifluoromethylated inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) that shows good results in anti-HIV chemotherapy.
      
Molecules 6f, i, and j inhibited only COX-1, and the disubstituted ethoxy derivative (6g) was inactive as a COX inhibitor (≤ 100?μM).
      
The study indicated that their antiproliferative activity is largely explained by the steric factors of the substituents, highlighting the role of the size and shape of the inhibitor in forming effective binding interactions with histone deacetylase.
      
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Although the occurence of a coenzyme I-independant, particle-bound α-glycerophosphate dehydrogenase in skeletal muscle of higher animals has long been recognized, little is known about its relation to the cytochrome system. Green has found that it is linked to cytochrome c but details of the electron transporting pathway has remained obscure. This problem has now been studied using the method of simultaneous action of two or more enzyme systems as described previously. Enzyme preparation obtained from thoroughly...

Although the occurence of a coenzyme I-independant, particle-bound α-glycerophosphate dehydrogenase in skeletal muscle of higher animals has long been recognized, little is known about its relation to the cytochrome system. Green has found that it is linked to cytochrome c but details of the electron transporting pathway has remained obscure. This problem has now been studied using the method of simultaneous action of two or more enzyme systems as described previously. Enzyme preparation obtained from thoroughly washed rabbit muscle mince has been employed in the present investigation. It has been found that in the presence of the rabbit muscle enzyme preparation, succinate and α-glycerophosphate each interferes with the rate of oxidation of the other when they are oxidized simultaneously. The inhibition of α-glycerophosphate oxidase by succinate can be reversed by the addition of pyrophosphate, a powerful inhibitor of succinic dehydrogenase. With cytochrome c as electron acceptor, the overall rate of simultaneous oxidation of α-glycerophosphate, succinate and reduced coenzyme I (CoIH) does not represent the sum of the rates of their separate oxidation, but corresponds only to the highest of the three rates, i.e. the rate of oxidation of CoIH. It is, therefore, believed that the α-glycerophosphate-, succinate- and CoIH-cytochrome c reductase systems have a common, velocity limiting electron carrier which is most probably the linking factor first proposed by Slater. In agreement with this conclusion, the α-glycerophosphate oxidase of rabbit muscle preparation has been found to be sensitive to the action of 2,3-dimercaptopropanol. Using 2,6-dichlorophenolindophenol, as acceptor, the overall rate of the simultaneous oxidation of succinate and α-glycerophosphate equals exacdy to the sum of the rates of their separate oxidation. Similar results have also been obtained even in presence of phenylurethane, which markedly inhibits the activity of succinic dehydrogenase and does not affect the activity of α-glycerophosphate dehydrogenase. These facts suggest that cytochrome b is not involved in the oxidation of α-glycerophosphate in rabbit muscle preparation. The pathway of hydrogen or electron transfer of the particulate α-glycerophosphate oxidase system may, therefore, be represented as follow: (See also Fig. 4)

(一) 在經徹底冲洗的兔骨骼肌製劑中,[L-α]甘油磷酸和琥珀酸的氧化彼此干涉。琥珀酸對[L-α]甘油磷酸氧化的抑制作用能因加入抑制琥珀酸脫氫酶的焦磷酸而解除。 (二) 當用細胞色素c作受體時[L-α]甘油磷酸,還原輔酶I和琥珀酸三者同時氧化時總氧化速度僅相當其中氧化速度最高者即還原輔酶I單獨氧化的速度。[L-α]甘油磷酸氧化酶系也因[2,3]二氫硫基丙醇的處理而失效。 (三) 當用[2,6]二氯酚靛酚作受體時[L-α]甘油磷酸和琥珀酸同時氧化時速度完全等於二底料單獨氧化時速度的和。[L-α]甘油磷酸的氧化不受苯代氨甲酸乙酯的影響。 (四) 本文結果說明[L-α]甘油磷酸的氧化不通過細胞色素b而通過中間因子和細胞色素c連接。

A method for the preparation of p-nitroacetophenone was developed on the principle of auto-oxidation of p-nitroethylbenzene. The product could be isolated in good quality by a process of simple freezing, Manganese acetate on calcium carbonate (1:10) was found to be the catalyst of choice. When a steady current of oxygen was bubbled through p-nitroethylbenzene at the rate of 0.55 ml. per minute for every gram of the mass, with stirring, at 140-145℃, and in the presence of catalyst equivalent to 0.005 to 0.01%...

A method for the preparation of p-nitroacetophenone was developed on the principle of auto-oxidation of p-nitroethylbenzene. The product could be isolated in good quality by a process of simple freezing, Manganese acetate on calcium carbonate (1:10) was found to be the catalyst of choice. When a steady current of oxygen was bubbled through p-nitroethylbenzene at the rate of 0.55 ml. per minute for every gram of the mass, with stirring, at 140-145℃, and in the presence of catalyst equivalent to 0.005 to 0.01% by weight of Mn~(++), p-nitroacetophenone content could be raised to a maximum of 62% within 18 to 30 hours. p-Nitrobenzoic acid and formic acid were also formed alongside with p-nitroacetophenone in an amount approximately 10% its weight, together with probably a trace of nitrophenols which was not identified. From 453 g. of p-nitroethylbenzene, after oxygenation and being chilled, the crude product separated and washed with a solution of sodium carbonate at 70-80℃ to remove p-nitrobenzoic acid, 153-161 g. of p-nitroacetophenone was obtained, m. p. 79-80℃. Unchanged p-nitroethylbenzene could be reclaimed from the mother liquor by fractionation. The role of calcium carbonate in the catalyst is, however, not only that of a neutral carrier. It was shown to exert an important moderating effect on the decomposition of the peroxide radical which was essential for the maintainance of auto-oxidation reaction chain. When manganese acetate alone was used as catalyst, the reaction was usually rapid at the onset but of short duration. "Besides, the reaction would then be very sensitive to the presence of even minute amounts of copper and iron salts which were both potent peroxide destroyers. The presence of calcium carbonate would bring to a check these deleterious effects, giving reaction liquor of light colour and high phenone content. An un-identified inhibitor was found to be formed and accumulated during the reaction.

發展了自对硝基乙苯經自动氧化以制取对硝基苯乙酮方法。产品可用冷冻法析出。最好的接触剂为附着于碳酸鈣上的醋酸錳(10:1).在攪拌下向对硝基乙苯中通氧,速度为每克每分鐘0.55ml.,温度140~145°C,接触剂用量相当于0.005~0.01%Mn~(++),在18至30小时內对硝基苯乙酮含量可达62%。接触剂中的碳酸鈣的作用,並非一單純的不活潑性載体。我們証明了:它具有延緩过氧化物分解的重要作用,而过氧化物的存在,对于自动氧化反应链锁的得以持续是必要的。它也能抵消可能存在于原料中的微量銅鹽和铁鹽对过氧化物的强力破坏作用,以得到酮含量高、色澤淺的产物。此外尚發現在反应过程中有一种未經証实的抑制物生成並积累。

(1) With the exception of EDTA and Na-azide most of the chelating agents were able to inhibit the activity of acylase. Under conditions of reversible inhibition the activity could be partially or completely restored by the addition of various metal ions. If the concentration of the inhibitor was kept at a chosen value, the extent of reactivation was found to depend on the concentration of the metal ions added. For each of these ions there was a definite and optimum concentration. It is suggested that the...

(1) With the exception of EDTA and Na-azide most of the chelating agents were able to inhibit the activity of acylase. Under conditions of reversible inhibition the activity could be partially or completely restored by the addition of various metal ions. If the concentration of the inhibitor was kept at a chosen value, the extent of reactivation was found to depend on the concentration of the metal ions added. For each of these ions there was a definite and optimum concentration. It is suggested that the metal ion needed for acylase activity may be Co~(++) or Mn~(++).

(1)大多数金属絡合剂除EDTA和迭氮化鈉外都能抑制酰化酶的活力,在可逆抑制情况下加入不同金属离子能部分或全部恢复酶活力。在固定絡合剂的浓度下酶活力的恢复程度与所加的金属离子浓度有关,每一金属离子都有一最适浓度。从以上結果推测酰化酶中的金属离子可能是Co~(++)或Mn~(++)离子。(2)在温和的条件下并有底物存在时,邻二氮菲和巯基乙酸对酰化酶的抑制是属于竞爭性,K_i值分別为1.28×10~(-4)M和1.74×10~(-3)M;一分子酶是与二分子抑制剂相結合。推測酰化酶可能是以二聚体形式存在。当抑制剂的浓度增大或使反应温度升高时都将引起不可逆的抑制。若酶与抑制剂預先一起保温亦得到类似的結果。(3)用电透析或在不同pH緩冲液下透析以除去酰化酶中的金属离子,都将导致酶的不可逆失活,因此酶中金属离子除起与底物結合的作用外,尚与維持蛋白貭的构型有关。

 
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