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Modulation of the TRPV4 ion channel as a therapeutic target for disease
- 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.
- Subjects :
- 0301 basic medicine
TRPV4
Lung Diseases
Pathology
medicine.medical_specialty
Gastrointestinal Diseases
Pain
TRPV Cation Channels
Disease
POTENTIAL VANILLOID 4
Lung injury
Bioinformatics
OBSTRUCTIVE PULMONARY-DISEASE
03 medical and health sciences
Transient receptor potential channel
ACTIVATED RECEPTOR-2
INFLAMMATORY BOWEL DISEASES
medicine
Animals
Edema
Humans
Pharmacology (medical)
Pharmacology & Pharmacy
CATION CHANNEL
Respiratory disease
Vascular tone
Pharmacology
Inflammation
COPD
Science & Technology
Chemistry
Gated Ion Channel
medicine.disease
Gastrointestinal disease
REGULATORY VOLUME DECREASE
AEROSOLIZED ADENOSINE 5'-TRIPHOSPHATE
ENDOTHELIAL-CELLS
CALCIUM INFLUX
Oedema
INDUCED LUNG INJURY
030104 developmental biology
Heart failure
1115 Pharmacology And Pharmaceutical Sciences
Animal studies
Life Sciences & Biomedicine
Subjects
Details
- ISSN :
- 1879016X
- Volume :
- 177
- Database :
- OpenAIRE
- Journal :
- Pharmacologytherapeutics
- Accession number :
- edsair.doi.dedup.....2386c7f3bd0f4b0857ed1d9dc0907696