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疾病中的经典瞬时受体电位通道:新型药物治疗的靶点?

Canonical transient receptor potential channels in disease: targets for novel drug therapy?

作者信息

Trebak Mohamed

机构信息

Department of Health and Human Services, National Institute of Environmental Health Sciences (NIEHS), NIH, Research Triangle Park, NC 27709, USA.

出版信息

Drug Discov Today. 2006 Oct;11(19-20):924-30. doi: 10.1016/j.drudis.2006.08.002. Epub 2006 Sep 7.

Abstract

The canonical transient receptor potential (TRPC) channels constitute one of the three major families within the large transient receptor potential (TRP) superfamily. TRPC channels are the closest mammalian homologues of Drosophila TRP, the light-activated channel in Drosophila photoreceptor cells. All TRPC channels (TRPC1-7) are activated via phospholipase-C-coupled receptors and were, therefore, proposed to encode elusive native receptor-activated cation channels in many cell types. A physiological role has been established for all of the known TRPC channels, including the control of vascular tone (TRPC1, TRPC4 and TRPC6) or lymphocyte activation, which is essential for immune competence (TRPC1 and TRPC3). The emergence of TRPC channels in controlling a variety of biological functions offers new and promising targets for drug development.

摘要

典型瞬时受体电位(TRPC)通道是大型瞬时受体电位(TRP)超家族中的三个主要家族之一。TRPC通道是果蝇TRP在哺乳动物中最接近的同源物,果蝇TRP是果蝇光感受器细胞中的光激活通道。所有TRPC通道(TRPC1 - 7)都通过磷脂酶C偶联受体激活,因此,有人提出它们在许多细胞类型中编码难以捉摸的天然受体激活阳离子通道。已经确定了所有已知TRPC通道的生理作用,包括对血管张力的控制(TRPC1、TRPC4和TRPC6)或淋巴细胞激活,这对免疫功能至关重要(TRPC1和TRPC3)。TRPC通道在控制多种生物学功能方面的出现为药物开发提供了新的、有前景的靶点。

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