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Current Topics in Medicinal Chemistry

Author(s): Masakazu Atobe*

DOI: 10.2174/1568026619666191010162850

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Activation of Transient Receptor Potential Vanilloid (TRPV) 4 as a Therapeutic Strategy in Osteoarthritis

Page: [2254 - 2267] Pages: 14

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Abstract

Transient receptor potential vanilloid (TRPV) 4 belongs to the TRPV subfamily of TRP ion channels. TRPV4 channels play a critical role in chondrocytes and thus TRPV4 is an attractive target of Disease-Modifying Osteoarthritis Drugs (DMOADs). Initial investigations of small molecules by Glaxo Smith Klein (GSK) as both agonists and antagonists via oral/intravenous administration have led to the use of existing agonists as lead compounds for biological studies. Our recent results suggest that local injection of a TRPV4 agonist is a potential treatment for osteoarthritis (OA). This review briefly summarizes updates regarding TRPV4 agonists based on recent advances in drug discovery, and particularly the local administration of TRPV4 agonists.

Keywords: Osteoarthritis, Anabolic effect, Intra-articular administration, Chondrocyte differentiation, Agonist, Short-term stimulation, Sox9.

Graphical Abstract

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