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Modulation of the TRPV4 ion channel as a therapeutic target for disease

Authors :
Maria G. Belvisi
Sara J. Bonvini
Peter McIntyre
Megan S. Grace
Source :
Pharmacologytherapeutics. 177
Publication Year :
2017

Abstract

Transient Receptor Potential Vanilloid 4 (TRPV4) is a broadly expressed, polymodally gated ion channel that plays an important role in many physiological and pathophysiological processes. TRPV4 knockout mice and several synthetic pharmacological compounds that selectively target TRPV4 are now available, which has allowed detailed investigation in to the therapeutic potential of this ion channel. Results from animal studies suggest that TRPV4 antagonism has therapeutic potential in oedema, pain, gastrointestinal disorders, and lung diseases such as cough, bronchoconstriction, pulmonary hypertension, and acute lung injury. A lack of observed side-effects in vivo has prompted a first-in-human trial for a TRPV4 antagonist in healthy participants and stable heart failure patients. If successful, this would open up an exciting new area of research for a multitude of TRPV4-related pathologies. This review will discuss the known roles of TRPV4 in disease, and highlight the possible implications of targeting this important cation channel for therapy.

Details

ISSN :
1879016X
Volume :
177
Database :
OpenAIRE
Journal :
Pharmacologytherapeutics
Accession number :
edsair.doi.dedup.....2386c7f3bd0f4b0857ed1d9dc0907696