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自50年前Monod、Wyman及Changeux最先提出用以解释酶学中蛋白及配体相互作用的变构调控学说以来,已经产生包括诱导-契合在内的多个调控模型及学说。随着生命科学的发展,这些理论被广泛应用于变构酶以及受体的变构调节现象研究中。Lefkowitz研究团队于1980年提出了揭示G蛋白偶联受体工作机制的三元复合体模型,为研究这一最大受体家族的变构调节位点和相关配体奠定了理论基础。着眼于配体与受体结合进而调控受体活化状态及功能的基础研究,已经对药物研发产生了重要的影响,并将进一步推动新型变构调节剂的开发。
Since Monod, Wyman and Changeux first proposed allosteric regulation of protein and ligand interactions in enzymology 50 years ago, a number of regulatory models and theories have been produced, including induction-fit. With the development of life science, these theories are widely used in the study of the allosteric regulation of allosteric enzymes and receptors. Lefkowitz’s research team put forward a ternary complex model to reveal the working mechanism of G protein-coupled receptors in 1980, which lays a theoretical foundation for the study of allosteric regulatory sites and related ligands of this largest receptor family. Focusing on the ligand and receptor binding and thus the activation of receptor activation status and function of the basic research has had an important impact on drug development and will further promote the development of new allosteric modulators.