Mechanistic insights of substrate transport and inhibitor binding revealed by high-resolution structures of human norepinephrine transporter  

作　　者：Ailong Song Xudong Wu 

机构地区：[1]Key Laboratory of Structural Biology of Zhejiang Province,School of Life Sciences,Westlake University,Hangzhou,Zhejiang,China [2]Westlake Laboratory of Life Sciences and Biomedicine,Hangzhou,Zhejiang,China [3]Institute of Biology,Westlake Institute for Advanced Study,Hangzhou,Zhejiang,China.

出　　处：《Cell Research》2024年第11期810-813,共4页细胞研究（英文版）

摘　　要：Dear Editor,Norepinephrine(NE),also known as noradrenaline,is an important neurotransmitter that plays crucial roles in the central nervous system,including the regulation of mood,memory,and alertness.It also functions as a key hormone in the whole body.In the brain,NE transporter(NET,encoded by the SLC6A2 gene),a Na+/Cl–-dependent transporter,reuptakes released NE at neuron synapses,thus maintaining NE homeostasis.Due to the important functions of NET,many drugs targeting NET have been developed to treat various neurological disorders.1 Despite previous efforts using NET surrogate to gain insights into the transport mechanism,2 the specific recognition of NE and the mechanistic details of the transport process remain elusive.Moreover,the binding modes of several FDA-approved NET-selective inhibitors require further investigations to provide a solid model for future structurebased drug discovery.

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分 类 号：Q51[生物学—生物化学]