Functionally deficient TRPV6 variants contribute to hereditary and familial chronic pancreatitis
Sign Up to like & getrecommendations! Published in 2021 at "Human Mutation"
DOI: 10.1002/humu.24315
Abstract: The recent discovery of TRPV6 as a pancreatitis susceptibility gene served to identify a novel mechanism of chronic pancreatitis (CP) due to Ca2+ dysregulation. Herein, we analyzed TRPV6 in 81 probands with hereditary CP (HCP),… read more here.
Keywords: functionally deficient; trpv6 variants; deficient trpv6; trpv6 ... See more keywords
A conserved gating element in TRPV6 channels.
Sign Up to like & getrecommendations! Published in 2017 at "Cell calcium"
DOI: 10.1016/j.ceca.2016.10.003
Abstract: The Ca2+-selective tetrameric Transient Receptor Potential Vanilloid 6 (TRPV6) channel is an inwardly rectifying ion channel. The constitutive current endures Ca2+-induced inactivation as a result of the activation of phospholipase C followed depletion of phosphatidylinositol… read more here.
Keywords: element trpv6; trpv6 channels; gating element; linker ... See more keywords
Photoswitchable Inhibitor of the Calcium Channel TRPV6.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00298
Abstract: Herein we report the first photoswitchable inhibitor of Transient Receptor Potential Vanilloid 6 (TRPV6), a selective calcium channel involved in a number of diseases and in cancer progression. By surveying analogs of a previously reported… read more here.
Keywords: photoswitchable inhibitor; calcium channel; trpv6; inhibitor calcium ... See more keywords
Structural bases of TRP channel TRPV6 allosteric modulation by 2-APB
Sign Up to like & getrecommendations! Published in 2018 at "Nature Communications"
DOI: 10.1038/s41467-018-04828-y
Abstract: Transient receptor potential (TRP) channels are involved in various physiological processes, including sensory transduction. The TRP channel TRPV6 mediates calcium uptake in epithelia and its expression is dramatically increased in numerous types of cancer. TRPV6… read more here.
Keywords: trp channels; trp channel; trpv6; allosteric modulation ... See more keywords
Inactivation-mimicking block of the epithelial calcium channel TRPV6
Sign Up to like & getrecommendations! Published in 2020 at "Science Advances"
DOI: 10.1126/sciadv.abe1508
Abstract: Small-molecule piperazine derivatives mimic inactivation by calmodulin to selectively and potently block TRPV6 channels. Epithelial calcium channel TRPV6 plays vital roles in calcium homeostasis, and its dysregulation is implicated in multifactorial diseases, including cancers. Here,… read more here.
Keywords: calcium channel; channel; epithelial calcium; inactivation ... See more keywords
Abstract 1936: The central role of NFAT signalling in the mechanism of action of the TRPV6 oncochannel inhibitor and clinical candidate SOR-C13
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1936
Abstract: SOR-C13, a 13-mer peptide derived from soricidin, the paralytic peptide in saliva of the Northern Short-tailed shrew, has completed an open-label, all comers Phase I Clinical Trial for the treatment of epithelially-derived cancers. SOR-C13 is… read more here.
Keywords: sor c13; role nfat; cancer; trpv6 ... See more keywords
TRPV6 deficiency attenuates stress and corticosterone-mediated exacerbation of alcohol-induced gut barrier dysfunction and systemic inflammation
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Immunology"
DOI: 10.3389/fimmu.2023.1093584
Abstract: Introduction Chronic stress is co-morbid with alcohol use disorder that feedback on one another, thus impeding recovery from both disorders. Stress and the stress hormone corticosterone aggravate alcohol-induced intestinal permeability and liver damage. However, the… read more here.
Keywords: trpv6; alcohol induced; alcohol; corticosterone ... See more keywords
TRPV6 Regulation by Cis-22a and Cholesterol
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12060804
Abstract: The highly calcium-selective transient receptor potential vanilloid-type channel TRPV6 is important for epithelial Ca2+ transport. Proper regulation of the inherently constitutively active TRPV6 channels is intricate in preserving Ca2+ homeostasis, whereby structural and functional data… read more here.
Keywords: trpv6 regulation; trpv6; cis 22a; cholesterol ... See more keywords
TRPV6 Calcium Channel Targeting by Antibodies Raised against Extracellular Epitopes Induces Prostate Cancer Cell Apoptosis
Sign Up to like & getrecommendations! Published in 2023 at "Cancers"
DOI: 10.3390/cancers15061825
Abstract: Simple Summary The TRPV6 channel is upregulated in many cancers and is associated with bad prognosis. Despite this fact, no reliable tool to target TRPV6 is known so far. Two prospective antibodies have been generated… read more here.
Keywords: cell; prostate cancer; trpv6 channel; trpv6 ... See more keywords
A Novel Anti-TRPV6 Antibody and Its Application in Cancer Diagnosis In Vitro
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24010419
Abstract: Though the first discovery of TRPV6 channel expression in various tissues took place in the early 2000s, reliable tools for its protein detection in various cells and tissues are still missing. Here we show the… read more here.
Keywords: trpv6 channel; anti trpv6; trpv6; cancer ... See more keywords
Intracellular Helix-Loop-Helix Domain Modulates Inactivation Kinetics of Mammalian TRPV5 and TRPV6 Channels
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24054470
Abstract: TRPV5 and TRPV6 are calcium-selective ion channels expressed at the apical membrane of epithelial cells. Important for systemic calcium (Ca2+) homeostasis, these channels are considered as gatekeepers of this cation transcellular transport. Intracellular Ca2+ exerts… read more here.
Keywords: inactivation kinetics; trpv6; helix; trpv5 trpv6 ... See more keywords