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糖皮质激素-受体相互作用的动力学。在缓慢平衡系统中测定的错误结合常数。

Kinetics of the glucocorticoid hormone-receptor interaction. False association constants determined in slowly equilibrating systems.

作者信息

Arányi P

出版信息

Biochim Biophys Acta. 1979 May 16;584(3):529-37. doi: 10.1016/0304-4165(79)90125-9.

DOI:10.1016/0304-4165(79)90125-9
PMID:454679
Abstract

The usual way of in vitro determination of association constants for hormone-receptor complexes is criticized. It is shown that if incubation time is short, relative to the half-life of the hormone-receptor complex, the value of the apparent Ka is proportional to the time of incubation. No sign of lack of equilibrium is apparent from the Scatchard plots. The case of rapidly denaturing receptor molecule is also discussed, with similar conclusions. Although terminology and examples are taken from the field of the glucocorticoid receptor research, all deductions are valid for other systems with similar association (and denaturation or monomolecular transformation) mechanisms and kinetic parameters.

摘要

体外测定激素-受体复合物结合常数的常用方法受到了批评。结果表明,如果孵育时间相对于激素-受体复合物的半衰期较短,表观解离常数(Ka)的值与孵育时间成正比。从Scatchard图中没有明显的平衡缺乏迹象。文中还讨论了受体分子快速变性的情况,得出了类似的结论。虽然术语和例子取自糖皮质激素受体研究领域,但所有推论对于具有相似结合(以及变性或单分子转化)机制和动力学参数的其他系统都是有效的。

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Kinetics of the glucocorticoid hormone-receptor interaction. False association constants determined in slowly equilibrating systems.糖皮质激素-受体相互作用的动力学。在缓慢平衡系统中测定的错误结合常数。
Biochim Biophys Acta. 1979 May 16;584(3):529-37. doi: 10.1016/0304-4165(79)90125-9.
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引用本文的文献

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Glucocorticoid--receptor interactions. Studies of the negative co-operativity induced by steroid interactions with a secondary, hydrophobic, binding site.糖皮质激素-受体相互作用。关于类固醇与第二个疏水结合位点相互作用所诱导的负协同性的研究。
Biochem J. 1980 Apr 15;188(1):237-45. doi: 10.1042/bj1880237.
2
Glucocorticoid-receptor interactions. Discrimination between glucocorticoid agonists and antagonists by means of receptor-binding kinetics.糖皮质激素受体相互作用。通过受体结合动力学区分糖皮质激素激动剂和拮抗剂。
Biochem J. 1982 Jun 15;204(3):721-9. doi: 10.1042/bj2040721.
3
Measurement of specific [3H]-ouabain binding to different types of human leucocytes.
测量特异性[³H]哇巴因与不同类型人类白细胞的结合。
Br J Clin Pharmacol. 1984 Aug;18(2):153-61. doi: 10.1111/j.1365-2125.1984.tb02447.x.