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首页> 外文期刊>Current drug targets. CNS and neurological disorders >GABA transporters and GABA-transaminase as drug targets.
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GABA transporters and GABA-transaminase as drug targets.

机译：GABA转运蛋白和GABA转氨酶作为药物靶标。

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The fine-tuning and homeostatic balance of the GABAergic inhibitory tone in the central nervous system (CNS) is a prerequisite for controlling the excitatory neurotransmission. This principal mechanism for controlling excitation is inhibition which has been the topic of intensive research covering all known functional entities of the GABAergic synapse. The therapeutical scope for targeting the GABA system covers a large number of neurological and psychiatric disorders. This review focuses on the major inactivation systems for GABAergic neurotransmission, the GABA transporters (GATs) and the GABA catabolic enzyme GABA -transaminase (GABA-T) as drug targets. Tiagabin and Vigabatrin, two anti-epileptic drugs on the market today, specifically inhibit GABA transport and metabolism, respectively. However, previous and recent evidence has clearly demonstrated the importance and differential functional roles of glial and neuronal GABA uptake and the metabolic fate of the sequestered neurotransmitter GABA in these cells. Moreover, the diverse expression patterns of the GABA transporters, in combination with development of GAT inhibitors with novel pharmacological profiles may initiate a renaissance for these inactivation systems as drugs targets. In particular, further research to elucidate the specialized physiological function of the GATs combined with their differential spatial expression could be of fundamental importance for the understanding of concerted action with regard to the fine-tuning of the GABAergic inhibitory tone. As such, selective targeting and modulation of GABA transporter subtypes and cell-specific GABA uptake and metabolism is of therapeutical interest in GABA-related CNS disorders, including epilepsy.
机译：中枢神经系统（CNS）中GABA能抑制音的微调和体内平衡是控制兴奋性神经传递的先决条件。控制兴奋的这种主要机制是抑制，这已成为涵盖GABA能突触的所有已知功能实体的深入研究的主题。靶向GABA系统的治疗范围涵盖了许多神经和精神疾病。这篇综述集中在主要的灭活系统为GABA能神经传递，GABA转运蛋白（GATs）和GABA分解代谢酶GABA转氨酶（GABA-T）作为药物靶标。当今市场上的两种抗癫痫药Tiagabin和Vigabatrin分别特异性抑制GABA转运和代谢。然而，先前和最近的证据已经清楚地证明了这些细胞中神经胶质和神经元GABA摄取以及隔离的神经递质GABA的代谢命运的重要性和不同的功能作用。此外，GABA转运蛋白的多种表达模式，与具有新颖药理学特征的GAT抑制剂的开发相结合，可能会引发这些灭活系统作为药物靶点的复兴。尤其是，进一步阐明GAT的特殊生理功能以及它们的差异空间表达，对于理解GABA能抑制音调的协调作用至关重要。因此，在包括癫痫在内的GABA相关的CNS疾病中，对GABA转运蛋白亚型的选择性靶向和调节以及细胞特异性GABA的摄取和代谢具有治疗意义。

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