Biochemical Neuropharmacology Laboratory, Kazan Federal University, 18 ul. Kremlevskaya, 420008 Kazan, Russia.
Int J Mol Sci. 2023 Aug 19;24(16):12973. doi: 10.3390/ijms241612973.
Partial reversible inhibition of enzymes, also called hyperbolic inhibition, is an uncommon mechanism of reversible inhibition, resulting from a productive enzyme-inhibitor complex. This type of inhibition can involve competitive, mixed, non-competitive and uncompetitive inhibitors. While full reversible inhibitors show linear plots for reciprocal enzyme initial velocity versus inhibitor concentration, partial inhibitors produce hyperbolic plots. Similarly, dose-response curves show residual fractional activity of enzymes at high doses. This article reviews the theory and methods of analysis and discusses the significance of this type of reversible enzyme inhibition in metabolic processes, and its implications in pharmacology and toxicology.
部分可逆抑制作用，也称双曲线抑制作用，是一种不常见的可逆抑制作用机制，由有活性的酶-抑制剂复合物产生。这种抑制作用可涉及竞争性、混合性、非竞争性和反竞争性抑制剂。虽然完全可逆抑制剂的酶初始速度与抑制剂浓度的倒数呈线性关系，但部分抑制剂产生双曲线关系。同样，剂量反应曲线显示高剂量下酶的剩余分数活性。本文综述了这种可逆酶抑制作用的理论和分析方法，并讨论了其在代谢过程中的意义，以及在药理学和毒理学中的意义。
