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Review of Transient Receptor Potential Canonical (TRPC5) Channel Modulators and Diseases.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-04-17 , DOI: 10.1021/acs.jmedchem.8b01954
Swagat Sharma 1 , Corey R Hopkins 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-04-17 , DOI: 10.1021/acs.jmedchem.8b01954
Swagat Sharma 1 , Corey R Hopkins 1
Affiliation
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Transient receptor potential canonical (TRPC) channels are highly homologous, nonselective cation channels that form many homo- and heterotetrameric channels. These channels are highly abundant in the brain and kidney and have been implicated in numerous diseases, such as depression, addiction, and chronic kidney disease, among others. Historically, there have been very few selective modulators of the TRPC family in order to fully understand their role in disease despite their physiological significance. However, that has changed recently and there has been a significant increase in interest in this family of channels which has led to the emergence of selective tool compounds, and even preclinical drug candidates, over the past few years. This review will cover these new advancements in the discovery of TRPC modulators and the emergence of newly reported structural information which will undoubtedly lead to even greater advancements.
中文翻译：
瞬态受体电位规范（TRPC5）通道调制器和疾病的综述。
瞬时受体电势规范（TRPC）通道是高度同源的非选择性阳离子通道，可形成许多同型和异四聚体通道。这些通道在脑和肾中高度丰富，并且与许多疾病有关，例如抑郁症，成瘾症和慢性肾脏病。从历史上看，尽管充分了解其在疾病中的作用，但TRPC家族的选择性调节剂很少，以充分了解其在疾病中的作用。但是，最近情况发生了变化，并且在过去几年中，对这一通道家族的兴趣显着增加，这导致了选择性工具化合物甚至临床前候选药物的出现。
更新日期：2019-04-03
中文翻译：
瞬态受体电位规范（TRPC5）通道调制器和疾病的综述。
瞬时受体电势规范（TRPC）通道是高度同源的非选择性阳离子通道，可形成许多同型和异四聚体通道。这些通道在脑和肾中高度丰富，并且与许多疾病有关，例如抑郁症，成瘾症和慢性肾脏病。从历史上看，尽管充分了解其在疾病中的作用，但TRPC家族的选择性调节剂很少，以充分了解其在疾病中的作用。但是，最近情况发生了变化，并且在过去几年中，对这一通道家族的兴趣显着增加，这导致了选择性工具化合物甚至临床前候选药物的出现。
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