Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease
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...
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MDPI AG
2018-06-01
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| Series: | Cells |
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| Online Access: | http://www.mdpi.com/2073-4409/7/6/52 |
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doaj-ddb1e4adaf8140b6991af15020d491c92020-11-24T23:05:56ZengMDPI AGCells2073-44092018-06-01765210.3390/cells7060052cells7060052Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and DiseaseAisling Minard0Claudia C. Bauer1David J. Wright2Hussein N. Rubaiy3Katsuhiko Muraki4David J. Beech5Robin S. Bon6School of Chemistry, University of Leeds, Leeds LS2 9JT, UKDepartment of Discovery and Translational Science, Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UKDepartment of Discovery and Translational Science, Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UKCentre for Atherothrombosis and Metabolic Disease, Hull York Medical School, Hull HU6 7RX, UKLaboratory of Cellular Pharmacology, School of Pharmacy, Aichi-Gakuin University, 1-100 Kusumoto, Chikusa, Nagoya 464-8650, JapanDepartment of Discovery and Translational Science, Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UKDepartment of Discovery and Translational Science, Leeds Institute of Cardiovascular and Metabolic Medicine, University of Leeds, Leeds LS2 9JT, UKProteins 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.http://www.mdpi.com/2073-4409/7/6/52ion channelTRPCsmall moleculescalciumchemical probes |
| collection |
DOAJ |
| language |
English |
| format |
Article |
| sources |
DOAJ |
| author |
Aisling Minard Claudia C. Bauer David J. Wright Hussein N. Rubaiy Katsuhiko Muraki David J. Beech Robin S. Bon |
| spellingShingle |
Aisling Minard Claudia C. Bauer David J. Wright Hussein N. Rubaiy Katsuhiko Muraki David J. Beech Robin S. Bon Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease Cells ion channel TRPC small molecules calcium chemical probes |
| author_facet |
Aisling Minard Claudia C. Bauer David J. Wright Hussein N. Rubaiy Katsuhiko Muraki David J. Beech Robin S. Bon |
| author_sort |
Aisling Minard |
| title |
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease |
| title_short |
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease |
| title_full |
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease |
| title_fullStr |
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease |
| title_full_unstemmed |
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease |
| title_sort |
remarkable progress with small-molecule modulation of trpc1/4/5 channels: implications for understanding the channels in health and disease |
| publisher |
MDPI AG |
| series |
Cells |
| issn |
2073-4409 |
| publishDate |
2018-06-01 |
| description |
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. |
| topic |
ion channel TRPC small molecules calcium chemical probes |
| url |
http://www.mdpi.com/2073-4409/7/6/52 |
| work_keys_str_mv |
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