The vanilloid transient receptor potential channel TRPV4: From structure to disease

• Published in: Progress in biophysics and molecular biology Vol. 103; no. 1; pp. 2 - 17
• Main Authors: Everaerts, Wouter, Nilius, Bernd, Owsianik, Grzegorz
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.09.2010
• Subjects: Animals; Bladder; Bone diseases; Bone Diseases - metabolism; Bone Diseases - pathology; Ca 2+ channels; Humans; Mechanosensor; Transient receptor potential; Transient Receptor Potential Channels - physiology; TRPV Cation Channels - chemistry; TRPV Cation Channels - metabolism; Urinary Bladder Diseases - metabolism; Urinary Bladder Diseases - pathology; Vanilloid receptor; Bladder; Vanilloid receptor; Bone diseases; Ca 2+ channels; Mechanosensor; Transient receptor potential
• ISSN: 0079-6107; 1873-1732; 1873-1732
• DOI: 10.1016/j.pbiomolbio.2009.10.002

The Transient Receptor Potential Vanilloid 4 channel, TRPV4, is a Ca 2+ and Mg 2+ permeable non-selective cation channel involved in many different cellular functions. It is activated by a variety of physical and chemical stimuli, including heat, mechano-stimuli, endogenous substances such as arachidonic acid and its cytochrome P450-derived metabolites (epoxyeicosatrienoic acids), endocannabinoids (anandamide and 2-arachidonoylglycerol), as well as synthetic α-phorbol derivatives. Recently, TRPV4 has been characterized as an important player modulating osteoclast differentiation in bone remodelling and as a urothelial mechanosensor that controls normal voiding. Several TRPV4 gain-of-function mutations are shown to cause autosomal-dominant bone dysplasias such as brachyolmia and Koszlowski disease. In this review we comprehensively describe the structural, biophysical and (patho)physiological properties of the TRPV4 channel and we summarize the current knowledge about the role of TRPV4 in the pathogenesis of several diseases.