TRPV5
Template:Cs1 config Template:Short description Template:Infobox gene Transient receptor potential cation channel subfamily V member 5 is a calcium channel protein that in humans is encoded by the TRPV5 gene.[1][2][3]
Function
The TRPV5 gene is a member of the transient receptor family and the TRPV subfamily. The calcium-selective channel, TRPV5, encoded by this gene has 6 transmembrane-spanning domains, multiple potential phosphorylation sites, an N-linked glycosylation site, and 5 ANK repeats. This protein forms homotetramers or heterotetramers and is activated by a low internal calcium level.[4]
Both TRPV5 and TRPV6 are expressed in kidney and intestinal epithelial cells.[5] TRPV5 is mainly expressed in kidney epithelial cells, where it plays an important role in the reabsorption of Ca2+,[6] whereas TRPV6 is mainly expressed in the intestine.[5] The enzyme α-klotho increases kidney calcium reabsorption by stabilizing TPRV5.[5] Klotho is a beta-glucuronidase-like enzyme that activates TRPV5 by removal of sialic acid.[7]
Clinical significance
Normally, about 95% to 98% of Ca2+ filtered from the blood by the kidney is reabsorbed by the kidney's renal tubule, mediated by TRPV5.[8] Genetic deletion of TRPV5 in mice leads to Ca2+ loss in the urine, and consequential hyperparathyroidism, and bone loss.[9]
Autosomal recessive hypercalciuria has been described in a family with a missense, inactivating genetic variant in TRPV5. This variant, known as p.(Val598Met), affects the TRP helix region of TRPV5, which is thought to control channel pore gating, assembly and protein folding.[10]
Inhibitors
- Econazole is a weak inhibitor of both TRPV5 and TRPV6, with an IC50 in the micromolar range
- ZINC17988990 is a potent and selective inhibitor of TRPV5, with an IC50 of 177nM and good selectivity over TRPV6 and the other TRPV channel subtypes.[11]
Interactions
TRPV5 has been shown to interact with S100A10.[12]
See also
References
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Further reading
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External links
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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