Transient receptor potential cation channel subfamily V members 2, 3, and 4 (TRPV2/3/4)

The TRPV2/TRPV3/TRPV4 group consists of three distinct non-selective cation channels within the vanilloid subfamily of the transient receptor potential (TRP) superfamily [1]. These channels are critical sensory transducers that respond to a variety of physical and chemical stimuli, including temperature, mechanical stress, and osmotic pressure [2]. TRPV2 is involved in high-threshold thermosensation and immune cell functions, while TRPV3 is predominantly expressed in skin keratinocytes where it regulates hair growth and barrier integrity [1, 3]. TRPV4 serves as a versatile mechanosensor and osmosensor, playing key roles in vascular tone, bone homeostasis, and lung fluid balance [2, 4]. Dysregulation of these channels is implicated in numerous pathologies, such as chronic pain, inflammatory skin diseases (e.g., atopic dermatitis), skeletal dysplasias, and pulmonary edema [3, 5]. Pharmacological modulation, particularly through small-molecule antagonists like GSK2798745, is a major area of drug development for treating respiratory, dermatological, and musculoskeletal disorders [5].

Other names

TRPV2TRPV3TRPV4Vanilloid receptor-like protein 1Vanilloid receptor-like protein 3Vanilloid receptor-like protein 2VRL-1VRL-3VRL-2OTRPC4VR-OACTRP12

These channels are primarily targeted by small-molecule antagonists to inhibit calcium influx and downstream signaling pathways associated with pain, inflammation, and fluid homeostasis. Some compounds, such as cannabidiol, act as agonists that can lead to channel desensitization, while others like tranilast specifically inhibit channel activity to treat allergic and inflammatory conditions.