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KMID : 0043320210440040354
Archives of Pharmacal Research
2021 Volume.44 No. 4 p.354 ~ p.377
Canonical transient receptor potential channels and their modulators: biology, pharmacology and therapeutic potentials
Gao Yuan-Yuan

Tian Wen
Zhang Hui-Nan
Sun Yang
Meng Jing-Ru
Cao Wei
Li Xiao-Qiang
Abstract
Canonical transient receptor potential channels (TRPCs) are nonselective, high calcium permeability cationic channels. The TRPCs family includes TRPC1, TRPC2, TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7. These channels are widely expressed in the cardiovascular and nervous systems and exist in many other human tissues and cell types, playing several crucial roles in the human physiological and pathological processes. Hence, the emergence of TRPCs modulators can help investigate these channels¡¯ applications in health and disease. It is worth noting that the TRPCs subfamilies have structural and functional similarities, which presents a significant difficulty in screening and discovering of TRPCs modulators. In the past few years, only a limited number of selective modulators of TRPCs were detected; thus, additional research on more potent and more selective TRPCs modulators is needed. The present review focuses on the striking desired therapeutic effects of TRPCs modulators, which provides intel on the structural modification of TRPCs modulators and further pharmacological research. Importantly, TRPCs modulators can significantly facilitate future studies of TRPCs and TRPCs related diseases.
KEYWORD
Canonical transient receptor potential channels modulators, Calcium ion, High-resolution structures, Drug discovery, Therapeutic potentials
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