
[生化] 竞争性抑制;竞争性抑制作用
The inhibition kinetic constant about competitive and non-competitive inhibition is figured out by calculating the substrate concentration on the same speed point.
竞争性抑制和非竞争性抑制通过求解等速点底物浓度的方法求解抑制常数。
Special competitive inhibition experiment demonstrated that foreign special DNA fragment inhibits the binding of the transcription factors with homologous fragments.
特异性竞争抑制试验表明外源性特异DNA片段能抑制相同片段与转录因子的结合。
In the competitive inhibition experiment, it showed that rapamycin and FK506 could bind this protein competitively and rapamycin had better binding capacity than FK506.
竞争性抑制实验显示雷帕霉素与FK506和该蛋白质的结合存在竞争性,且雷帕霉素与该蛋白质的结合能力比FK506强。
Meanwhile, many drugs can influence the activity of CYP2D6 by competitive inhibition or induction, which is easy to cause interaction in coadministration.
而且CYP2D6能被多种药物竞争性抑制和诱导,药物联用时易产生相互作用。
METHODS The paratope mapping of antibo***s was determined by competitive inhibition in radioimmunoassay and the sequences of variable regions among the antibo***s were compared.
应用放射免疫竞争抑制试验测定抗体的配位特异性,并对抗体的可变区序列进行比较。
Competitive inhibition between methane and propene was minimized by physical separation of the regeneration and epoxidation.
将再生和环氧化过程分开进行,以减小甲烷和丙烯的竞争抑制。
QU exhibited competitive inhibition of CYP3A2 dextromethorphan N-demethylation reaction and expressed noncompetitive inhibition of CYP2E1 chlorzoxazone-6-hydroxylation reaction.
槲皮素竞争性抑制CYP3A2右美沙芬N脱甲基反应,非竞争性抑制CYP2E1氯唑沙宗6羟化反应。
COMPETITIVE INHIBITION Competitive inhibitors compete with substrate for an enzyme's active site, lowering the enzyme's likelihood of binding substrate and slowing the observed reaction velocity.
竞争性抑制竞争性抑制剂与底物竞争酶的活性部位,降低酶的约束力基板的可能性,并观察到的反应速 度放缓。
The effects of competitive product inhibition are shown to increase the substrate concentration in the carrier, and, additionally, to increase the effectiveness factors slightly.
产物竞争性抑制的存在将增加载体颗粒内的底物浓度,对效率因子的影响较小。
A kinetics model was developed for predicting and simulating immobilized cellulase performance, which follows Michaelis_Menten kinetics with competitive product inhibition.
建立了固定化纤维素酶的反应动力学模型,该模型以米氏方程为基础并考虑了产物竞争性抑制的影响。
Kinetic stu***s showed that the mechanism of tyrosinase inhibition of both mono-demethoxycurcumin and carboxylized curcumin belongs to non-competitive type inhibition.
抑制动力学研究表明,单去*********姜黄素及带羧基的姜黄素衍生物对酪氨酸酶的抑制均属于非竞争性抑制类型。
Kinetic stu***s of AG114 inhibition on recombinant human CK2 showed that the inhibition was mixed competitive with GTP and noncompetitive with casein.
AG114对重组人CK2的动力学研究表明:它与GTP呈混合竞争性抑制作用,与酪蛋白呈非竞争性抑制作用。
Kinetic stu***s of AG34 on recombinant human CK2 showed that the inhibition was mixed (competitive is dominant) with GTP and noncompetitive with casein.
AG34对重组人CK2的动力学研究表明:它与GTP呈现以竞争性为主的混合型抑制作用,与酪蛋白呈非竞争性抑制作用。
Kinetic stu***s of AG1112 on recombinant human CK2 showed that the inhibition was mixed(competitive is dominant) with GTP and noncompetitive with casein.
AG1112对重组人CK2的动力学研究表明:它与GTP和酪蛋白分别呈混合性和非竞争性抑制作用。
It has been found that the coupling process is more effective for eliminating the product noncompetitive inhibition compared with the competitive one.
结果表明,该耦合过程对产物非竞争性抑制的消除效果要优于竞争性抑制。
The inhibition of AG372 on recombinant human CK2 was competitive with GTP and noncompetitive with casein.
AG372对重组人CK2的动力学研究表明:它与GTP呈竞争性抑制作用,与酪蛋白呈非竞争性抑制作用。
Kinetic analysis revealed that the inhibition on chymotrypsin by S-24 enzyme inhibitor is competitive with respect to the substrate.
动力学研究表明S-24酶抑制剂抑制糜蛋白酶,对底物酪蛋白、血红蛋白的关系均为竟争性抑制。
Competitive kinetics Kinetic stu***s can be used to determine the type and potency of inhibition for an unknown inhibitor.
竞争动力学可用于动力学研究,以确定一个未知抑制剂抑制的类型和效力。
Methods: The colloidal gold strip for specific sulfadimidine was developed successfully on the basis of competitive inhibition immunochromatography mechanism.
方法:应用竞争抑制免疫层析原理,研制磺胺*********嘧啶胶体金试纸条。
竞争性抑制(competitive inhibition)是酶动力学中的一种抑制作用机制,指抑制剂分子与酶的正常底物在结构上相似,两者通过竞争结合酶的活性位点,从而降低酶的催化效率。这种抑制作用的特点体现在米氏方程的变化上:抑制剂的加入会使底物的表观米氏常数((Km))增大,而最大反应速率((V{max}))保持不变,公式可表示为: $$ V0 = frac{V{max}[S]}{K_m(1 + [I]/K_i) + [S]} $$ 其中([I])为抑制剂浓度,(K_i)为抑制常数。
一个经典案例是磺胺类药物对细菌二氢叶酸合成酶的抑制。磺胺分子与底物对氨基苯甲酸(PABA)结构相似,通过占据酶的活性中心阻断细菌叶酸合成途径,从而抑制其增殖。在代谢调控中,此类抑制作用常见于反馈抑制机制,例如终产物通过竞争性抑制调控代谢通路关键酶活性。
现代药物研发高度依赖该原理,如他汀类药物通过竞争性抑制HMG-CoA还原酶降低胆固醇合成。这种靶向作用机制因其可逆性和特异性,成为设计选择性抑制剂的重要策略。
竞争性抑制(competitive inhibition)是酶催化反应中的一种抑制作用机制,其核心特征如下:
作用机制 抑制剂与底物结构相似,两者竞争结合酶的活性位点。当抑制剂占据活性位点时,底物无法与酶结合,导致催化反应速率降低。这种抑制可通过增加底物浓度来逆转。
动力学参数变化
经典案例 丙二酸对琥珀酸脱氢酶的抑制是典型例子。丙二酸与底物琥珀酸结构相似,通过竞争结合酶活性位点阻断三羧酸循环。
应用领域 药物开发中广泛应用此原理,例如:
该机制揭示了生物分子间相互作用的特异性,为代谢调控和药物靶点设计提供了理论基础。
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