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人类微量胺相关受体1激活的分子基础

Gregory Zilberg¹, Alexandra K Parpounas², Audrey L Warren²

¹Department of Neuroscience, Icahn School of Medicine at Mount Sinai, New York, New York 10029.

bioRxiv : the preprint server for biology

|November 21, 2023

概括

研究人员阐明了人类的微氨基关联受体1 (hTAAR1) 结构,揭示了它的功能和药理学. 这项研究揭示了非目标药物活动,并提供了对hTAAR1的见解.

科学领域:

神经科学是一个神经科学.
分子生物学分子生物学
药理学药理学是指药理学的学科.

背景情况:

人类的微氨基关联受体1 (hTAAR1) 调节单氨基神经传递和精神刺激作用.
它的分子激活机制和与动物对应物之间的药理差异尚不清楚,这阻碍了药物开发.

研究的目的:

为了阐明hTAAR1激活的分子机制.
调查人类和动物TA1药理差异的结构基础.
为了确定与hTAAR1.1.的新药相互作用.

主要方法:

确定了人体TA1受体与Gαs异构分离体结合的结构.
进行局部定向突变发生,以改变受体选择性.
研究了将残留物替换为相关单氨基受体的残留物的影响.
评估了asenapine在hTAAR1.1上的活性.

主要成果:

hTAAR1的结构揭示了与其他TAAR和5-HT4R血清素共享的元素.
一个单一的突变显著转移hTAAR1的选择性向动物的ortologs.
阿塞纳是一种非典型的抗精神病药物,被确定为一种强大的hTAAR1激活剂.
结构和功能的比较突出显示了hTAAR1与其正义基因之间的差异.

结论:

提供了关于hTAAR1结构,功能和药理学的详细见解.
这项研究将hTAAR1的分子药理与相关受体进行对比.
在hTAAR1上发现了单氨基药物 (包括asenapine) 的非向活性.

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