Dunlop John, Butera John A
Neuroscience Discovery Research, Wyeth Research, CN 8000, Princeton NJ 08543, USA.
Curr Top Med Chem. 2006;6(17):1897-906. doi: 10.2174/156802606778249829.
This review provides an overview of ligands for the excitatory amino acid transporters (EAATs), a family of high-affinity glutamate transporters localized to the plasma membrane of neurons and astroglial cells. Ligand development from the perspective of identifying novel and more selective tools for elucidating transporter subtype function, and the potential of transporter ligands in a therapeutic setting are discussed. Acute pharmacological modulation of EAAT activity in the form of linear and conformationally restricted glutamate and aspartate analogs is presented, in addition to recent strategies aimed more toward modulating transporter expression levels, the latter of particular significance to the development of transporter based therapeutics.
本综述概述了兴奋性氨基酸转运体（EAATs）的配体，EAATs是一类高亲和力的谷氨酸转运体家族，定位于神经元和星形胶质细胞的质膜。从鉴定用于阐明转运体亚型功能的新型且更具选择性的工具的角度讨论了配体开发，以及转运体配体在治疗环境中的潜力。除了最近更倾向于调节转运体表达水平的策略（后者对基于转运体的治疗方法的开发尤为重要）之外，还介绍了以线性和构象受限的谷氨酸和天冬氨酸类似物形式对EAAT活性进行的急性药理学调节。
