The solute carrier family 18 member 2 (SLC18A2) also known as vesicular monoamine transporter 2 (VMAT2) is a protein that in humans is encoded by the SLC18A2 gene. [5] VMAT2 is an integral membrane protein that transports monoamines —particularly neurotransmitters such as dopamine , norepinephrine , serotonin , and histamine —from cellular ...

2023年11月1日 · Vesicular monoamine transporter 2 (VMAT2) accumulates monoamines in presynaptic vesicles for storage and exocytotic release, and has a vital role in monoaminergic...

2019年4月2日 · The vesicular monoamine transporter type 2 (VMAT2) inhibitors are agents that cause a depletion of neuroactive peptides such as dopamine in nerve terminals and are used to treat chorea due to neurodegenerative diseases (such as Huntington chorea) or dyskinesias due to neuroleptic medications (tardive dyskinesia).

2023年11月1日 · Here we report cryo-electron microscopy structures of the human vesicular monoamine transporter VMAT2 in complex with the antichorea drug tetrabenazine, the antihypertensive drug reserpine or the...

2024年1月2日 · VMAT2 inhibitors reserpine and tetrabenazine are used to treat hypertension, movement disorders associated with Huntington’s Disease and Tardive Dyskinesia.

A protein called VMAT2 controls how much chemical messenger is stored in the nerve cell and how much is released. The VMAT2 inhibitors blocks VMAT2 which means there is a lower amount of neurotransmitter available and therefore reduces the unwanted body movements.

2023年11月16日 · 在哺乳动物中已鉴定出两个 vmat 蛋白家族成员： vmat1 ( slc18a1 ) 和 vmat2 ( slc18a2 ) 。 vmat1 主要在外周内分泌细胞中表达， vmat2 则表达更为广泛，并且作为负责神经元单胺转运

2023年12月12日 · 该研究为理解vmat2的底物识别、药物抑制、质子耦合转运过程等分子机制奠定了重要的结构基础，并为开发靶向vmat2的构象特异性以及亚型特异性药物提供了重要的结构信息。

2023年11月2日 · 该工作首次报道了人源vmat2蛋白结合抑制剂tbz、rsp及其底物5-羟色胺（5-ht）的冷冻电镜结构，揭示了两种抑制剂发挥功能以及vmat2转运底物的分子机制 ...

2025年1月2日 · Vesicular monoamine transporter 2 (VMAT2) is crucial for packaging monoamine neurotransmitters into synaptic vesicles, with their dysregulation linked to schizophrenia, mood disorders, and Parkinson's disease. Tetrabenazine (TBZ) and valbenazine (VBZ), both FDA-approved VMAT2 inhibitors, are employe …