In vivo significance of kinetic constants of macromolecular proteinase inhibitors.
In vivo significance of kinetic constants of macromolecular proteinase inhibitors.
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大分子蛋白酶抑制剂动力学常数的体内意义。
DOI：
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发表时间：
1984
影响因子：
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通讯作者：
J. Bieth
中科院分区：
文献类型：
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作者：
J. Bieth
许多生理和病理过程由蛋白酶控制，蛋白酶的活性本身由大分子抑制剂控制。近年来，越来越多的研究人员对在生物体液或组织中寻找新的抑制剂感兴趣。通常认为，如果此类抑制剂在体外具有活性，则它们在体内也将具有活性。但情况并非总是如此。为了确定抑制剂是否发挥生理作用，需要两组数据：体内抑制剂浓度和描述蛋白酶/抑制剂相互作用的动力学参数。本文简要介绍了这些参数，它们的测量和定义蛋白酶抑制剂在健康和疾病中的作用。
Many physiological and pathological processes are controlled by proteinases whose activity is itself controlled by macromolecular inhibitors. In recent years a growing number of investigators have been interested in searching for novel inhibitors in biological fluids or tissues. It is commonly thought that if such inhibitors are active in vitro, they will also be active in vivo. This is not always the case. To decide whether an inhibitor plays a physiological role or not, two sets of data are required: the in vivo inhibitor concentration and the kinetic parameters describing the proteinase/inhibitor interaction. This paper describes briefly these parameters, their measurement and their use for defining the role of proteinase inhibitors in health and disease.