Dissecting TRPV1: Lessons to be learned?

The transient receptor potential channel TRPV1 is a polymodal nociceptor. It is primarily expressed in dorsal root ganglia and peripheral sensory nerve endings, and to a much lesser extent, in the central nervous system. It has also been implicated in the functional properties of e.g. urinary and br...

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Bibliographic Details
Published in:Channels (Austin, Tex.) Tex.), 2011-05, Vol.5 (3), p.201-204
Main Authors: Grimm, Christian, Aneiros, Eduardo, de Groot, Marcel
Format: Article
Language:English
Subjects:
Animals
Binding
Biology
Bioscience
Calcium
Cancer
Capsaicin - pharmacology
Cell
Cycle
Drug Delivery Systems
Fever - genetics
Fever - metabolism
Ganglia, Spinal - metabolism
Hot Temperature
Landes
Nociceptors - metabolism
Organogenesis
Pain - drug therapy
Pain - metabolism
Proteins
Protons
Respiratory Mucosa - metabolism
Species Specificity
TRPV Cation Channels - agonists
TRPV Cation Channels - antagonists & inhibitors
TRPV Cation Channels - genetics
TRPV Cation Channels - metabolism
Urothelium - metabolism
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Summary:The transient receptor potential channel TRPV1 is a polymodal nociceptor. It is primarily expressed in dorsal root ganglia and peripheral sensory nerve endings, and to a much lesser extent, in the central nervous system. It has also been implicated in the functional properties of e.g. urinary and bronchial epithelia. TRPV1 has long been under intensive investigation by the pharmaceutical industry as a candidate drug target especially for pain conditions. This review summarizes the current knowledge of the molecular determinants of TRPV1 channel activation by heat, protons and capsaicin. Newly discovered heat and proton activation sites within the pore domain are discussed as well as potential consequences for drug discovery. Polymodal TRPV1 antagonists were found to cause hyperthermia in a species-dependent manner in-vivo, hence the discovery of euthermic compounds with an appropriate modality selectivity profile will be crucial for TRPV1's future as a drug target.
ISSN:1933-6950
1933-6969
DOI:10.4161/chan.5.3.16291