Pin J P, De Colle C, Bessis A S, Acher F
Centre INSERM-CNRS de Pharmacologie-Endocrinologie, UPR 9023-CNRS, Laboratoire des Mécanismes Moléculaires des Communications Cellulaires, Montpellier, France.
Eur J Pharmacol. 1999 Jun 30;375(1-3):277-94. doi: 10.1016/s0014-2999(99)00258-7.
The metabotropic glutamate receptors are GTP-binding-protein (G-protein) coupled receptors that play important roles in regulating the activity of many synapses in the central nervous system. As such, these receptors are involved in a wide number of physiological and pathological processes. Within the last few years, new potent and selective agonists and antagonists as well as radioligands acting on these receptors have been developed. Molecular modeling studies revealed the structural features of the glutamate binding site, and will be useful for the design of more selective and potent ligands. More interestingly, recent data revealed new regulatory sites on the receptor protein, able either to decrease or potentiate the action of the endogenous ligand. No doubt that in the near future a multitude of new tools to modulate the activity of these receptors will be discovered, enabling the identification of the possible therapeutic applications for these new neuroactive molecules.
代谢型谷氨酸受体是与GTP结合蛋白（G蛋白）偶联的受体，在调节中枢神经系统中许多突触的活性方面发挥着重要作用。因此，这些受体参与了大量的生理和病理过程。在过去几年中，已经开发出作用于这些受体的新型强效和选择性激动剂、拮抗剂以及放射性配体。分子建模研究揭示了谷氨酸结合位点的结构特征，这将有助于设计更具选择性和强效的配体。更有趣的是，最近的数据揭示了受体蛋白上的新调节位点，这些位点能够降低或增强内源性配体的作用。毫无疑问，在不久的将来将会发现大量调节这些受体活性的新工具，从而能够确定这些新型神经活性分子可能的治疗应用。
