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INTRINSIC ACTIVITY AT THE MOLECULAR LEVEL - ARIENS,E.J. CONCEPT VISUALIZED

机译：分子水平的内在活动-ARIENS，E.J。可视化的概念

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The concept of using affinity and intrinsic activity to analyze drug interactions with receptors has had a long history in pharmacological studies. In the simplest case, the biological response will be proportional to the amount of drug bound, i.e. its affinity However, the biological response is also mediated by the ability of a drug when bound to exert its maximum effectiveness. This effectiveness is termed the intrinsic activity Physicochemical processes have been thought to be at the basis of intrinsic activity Detailed oxygen and solution binding experiments combined with X-ray crystallographic studies on allosteric effecters to hemoglobin demonstrate that these potential drug agents bind at the same site in hemoglobin with similar binding constants yet shift the allosteric equilibrium and the oxygen affinity of the T-structure by different degrees. Therefore some of the effecters with similar binding affinities for the same site exhibit varying degrees of affectiveness, i.e. they possess different intrinsic activities. The intrinsic activity of the effector is defined as the ratio of the oxygen affinity constant to the T-state with drug/oxygen affinity constant to the T-state without drug (K-T+drug)/(K-Tcontrol) The source of the intrinsic activity appears to be the ability of the effecters to interact with key residues such as Lys99 alpha at the binding site. These results suggest a general molecular mechanism for allosteric effector modulation of hemoglobin function that might be of use in other allosteric enzyme systems. [References: 38]
机译：在药理学研究中，使用亲和力和内在活性分析药物与受体相互作用的概念已有很长的历史。在最简单的情况下，生物学反应将与所结合的药物的量成比例，即其亲和力。然而，生物学反应还由药物在结合时发挥其最大功效的能力来介导。这种有效性被称为内在活性。物理化学过程被认为是内在活性的基础。详细的氧气和溶液结合实验，以及对变构效应物与血红蛋白的X射线晶体学研究表明，这些潜在的药物在相同部位结合。具有相似结合常数的血红蛋白可将变构平衡和T结构的氧亲和力移动不同程度。因此，对于相同位点具有相似结合亲和力的一些效应子表现出不同程度的情感性，即它们具有不同的内在活性。效应子的内在活性定义为具有药物的氧亲和常数与T状态的比值/不含药物的K态相对于T状态的比值（K-T + drug）/（K-Tcontrol）内在活性似乎是效应子在结合位点与关键残基如Lys99 alpha相互作用的能力。这些结果提示了对血红蛋白功能的变构效应子调节的一般分子机制，该分子机制可能在其他变构酶系统中使用。 [参考：38]

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