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Cells 2018, 7(6), 52; https://doi.org/10.3390/cells7060052

Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease

1
School of Chemistry, University of Leeds, Leeds LS2 9JT, UK
2
Department of Discovery and Translational Science, Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UK
3
Centre for Atherothrombosis and Metabolic Disease, Hull York Medical School, Hull HU6 7RX, UK
4
Laboratory of Cellular Pharmacology, School of Pharmacy, Aichi-Gakuin University, 1-100 Kusumoto, Chikusa, Nagoya 464-8650, Japan
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 27 April 2018 / Revised: 21 May 2018 / Accepted: 23 May 2018 / Published: 1 June 2018
(This article belongs to the Special Issue TRP Channels in Health and Disease)
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Abstract

Proteins of the TRPC family can form many homo- and heterotetrameric cation channels permeable to Na+, K+ and Ca2+. In this review, we focus on channels formed by the isoforms TRPC1, TRPC4 and TRPC5. We review evidence for the formation of different TRPC1/4/5 tetramers, give an overview of recently developed small-molecule TRPC1/4/5 activators and inhibitors, highlight examples of biological roles of TRPC1/4/5 channels in different tissues and pathologies, and discuss how high-quality chemical probes of TRPC1/4/5 modulators can be used to understand the involvement of TRPC1/4/5 channels in physiological and pathophysiological processes. View Full-Text
Keywords: ion channel; TRPC; small molecules; calcium; chemical probes ion channel; TRPC; small molecules; calcium; chemical probes
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Minard, A.; Bauer, C.C.; Wright, D.J.; Rubaiy, H.N.; Muraki, K.; Beech, D.J.; Bon, R.S. Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease. Cells 2018, 7, 52.

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