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Structural insights into the gating mechanisms of TRPV channels
Affiliation:1. Department of Urology, CHU-Universite de Brest, Brest 29000, France;2. Department of Urology, CHU-Universite de Tours, Tours 37000, France;3. Department of Urology, Institut Mutualiste Montsouris, Paris 75014, France;4. Inserm U1069, Tours 37000, France;5. Department of Pathology, CHU-Universite de Tours, Tours 37000, France;1. Weill Cornell Medicine in Qatar, Qatar Foundation — Education City, Doha, Qatar;2. Division of Clinical Nutrition, Faculty of Home Economics, Kyoritsu Women''s University, Tokyo, Japan;3. Laboratory of Neuroendocrinology, I.P. Pavlov Institute of Physiology, Russian Academy of Sciences, St. Petersburg, Russia;4. Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic;5. Department of Pharmacology and Toxicology, Faculty of Pharmacy, Comenius University, Bratislava, Slovak Republic;6. Laboratory of Structural Biology and Proteomics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech Republic;7. nd;1. Department of Chemistry, King''s College London, Britannia House, 7 Trinity Street, London SE1 1DB, UK;2. Department of Medical Biotechnologies, University of Siena, Viale Mario Bracci 16, I-53100 Siena, Italy;3. Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford OX1 3TA, UK
Abstract:Transient Receptor Potential channels from the vanilloid subfamily (TRPV) are a group of cation channels modulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. Their roles in human health make them of keen interest, particularly from a pharmacological perspective. However, despite this interest, the complexity of these channels has made it difficult to obtain high resolution structures until recently. With the cryo-EM resolution revolution, TRPV channel structural biology has blossomed to produce dozens of structures, covering every TRPV family member and a variety of approaches to examining channel modulation. Here, we review all currently available TRPV structures and the mechanistic insights into gating that they reveal.
Keywords:Ion channels  TRPV  Cryo-EM  X-ray crystallography  TRP channels
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