The transient receptor potential (TRP) superfamily is diverse, encoded by 28 TRP channel genes and grouped into six subfamilies: TRPC (canonical), TRPV (vanilloid), TRPM (melastatin), TRPA (ankyrin), TRPP (polycystin), and TRPML (mucolipin). The vanilloid subfamily (TRPV) was named after the founding of its member, the vanilloid (capsaicin) receptor TRPV1. Now, five other members of this family have been identified. Structurally, these TRPV channels monomeric subunit components each contains six transmembrane domains (designated S1-S6) with a pore domain between S5 and S6 segments. The N-terminus of TRPV channels contains six ankyrin repeats.
TRPV1-4 channels are thermosensitive but have different temperature activation profiles. TRPV1, V3, and V4 are expressed in nociceptive sensory neurons in the central nervous system and thus are involved in the generation and transduction of pain. TRPV5 and TRPV6 are calcium-selective channels that are mainly distributed in the intestine and kidney. Dysfunction of TRPV channels has been implicated in various disease states ranging from chronic pain and overactive bladder (TRPV1) through obesity (TRPV4), diabetes (TRPV1), chronic cough (TRPV1), and chronic obstructive pulmonary disease (COPD; TRPV4) to dermatological disorders (TRPV3 in Olmsted Syndrome) and cancer (TRPV2). Clinically, a number of potent, small-molecule TRPV1 and TRPV3 antagonists have already entered clinical trials as novel analgesic agents. With the increasing understanding of the TRPV functions in disease and health, more progress will be made in the drug discovery of new disease areas.
Here, we give an introduction of human TRPV channel members regarding their function, tissue distribution, selectivity, clinical significance, and potential as drug targets.
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