Erratum to: First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors

Fu, Siqing; Hirte, Hal W.; Welch, Sarah; Ilenchuk, T. Toney; Lutes, Tyler; Rice, Claire M; Fields, N; Nemet, A.; Dugourd, Dominique; Piha-Paul, Sarina A.; Subbiah, Vivek; Liu, L.; Gong, Jing; Hong, Deng; Stewart, John M.

doi:10.1007/s10637-017-0455-y

Cited by 10 publications

(6 citation statements)

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“…A number of TRPV6 inhibitors have already shown potential in reducing cell growth f.i. in breast cancer models [63][64][65][66][67] . Whether these same inhibitors also impact EMT, needs to be studied.…”

Section: Discussionmentioning

confidence: 99%

TRPV6 calcium channel directs homeostasis of the mammary epithelial sheets and controls epithelial mesenchymal transition

Kärki

Rajakylä

Acheva

et al. 2020

Sci Rep

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Epithelial integrity is lost upon cancer progression as cancer cells detach from the primary tumor site and start to invade to the surrounding tissues. Invasive cancers of epithelial origin often express altered levels of TRP-family cation channels. Upregulation of TRPV6 Ca2+-channel has been associated with a number of human malignancies and its high expression in breast cancer has been linked to both proliferation and invasive disease. The mechanisms behind the potential of TRPV6 to induce invasive progression have, however, not been well elucidated. Here we show that TRPV6 is connected to both E-cadherin-based adherens junctions and intracellular cytoskeletal structures. Loss of TRPV6 from normal mammary epithelial cells led to disruption of epithelial integrity and abnormal 3D-mammo sphere morphology. Furthermore, expression level of TRPV6 was tightly linked to the levels of common EMT markers, suggesting that TRPV6 may have a role in the mesenchymal invasion of breast cancer cells. Thus, either too low or too high TRPV6 levels compromise homeostasis of the mammary epithelial sheets and may promote the progression of pathophysiological conditions.

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Section: Discussionmentioning

confidence: 99%

TRPV6 calcium channel directs homeostasis of the mammary epithelial sheets and controls epithelial mesenchymal transition

Kärki

Rajakylä

Acheva

et al. 2020

Sci Rep

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“…Reducing TRPV6 protein production in pancreatic cell lines with siRNA reduced proliferation and invasion, and initiated apoptosis and cell cycle arrest 102. In a Phase I clinical trial of a peptide inhibitor of TRPV6 activity two patients with advanced pancreatic cancers showed tumour reduction (one by -27% by RECIST criteria) with one patient showing 55% decrease in the validated pancreatic cancer biomarker CA19-9 103. Of the 23 patients enrolled in this study with cancers classed as “TRPV6-rich” >50% showed stable disease after two courses of treatment with no drug-related serious adverse events.…”

Section: Introductionmentioning

confidence: 99%

“…A review of pharmacological approaches to exploiting TRP channel activity in cancer has been published 164 and a number of TRPV6 inhibitors are cited in a recent review of targeting calcium signalling in cancer 79. A peptide inhibitor of TRPV6 (SOR-C13) completed a Phase I clinical safety trial 103 and has been shown to reduce growth in cell and animal models ovarian and prostate cancers 100, 101. Table 3 summarizes the public literature for inhibitors of TRPV6 and TRPV5.…”

Section: Introductionmentioning

confidence: 99%

TRPV6 as A Target for Cancer Therapy

Stewart¹

2020

J. Cancer

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Two decades ago a class of ion channels, hitherto unsuspected, was discovered. In mammals these Transient Receptor Potential channels (TRPs) have not only expanded in number (to 26 functional channels) but also expanded the view of our interface with the physical and chemical environment. Some are heat and cold sensors while others monitor endogenous and/or exogenous chemical signals. Some TRP channels monitor osmotic potential, and others measure cell movement, stretching, and fluid flow. Many TRP channels are major players in nociception and integration of pain signals. One member of the vanilloid sub-family of channels is TRPV6. This channel is highly selective for divalent cations, particularly calcium, and plays a part in general whole-body calcium homeostasis, capturing calcium in the gut from the diet. TRPV6 can be greatly elevated in a number of cancers deriving from epithelia and considerable study has been made of its role in the cancer phenotype where calcium control is dysfunctional. This review compiles and updates recent published work on TRPV6 as a promising drug target in a number of cancers including those afflicting breast, ovarian, prostate and pancreatic tissues.

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“…Prostate and ovarian cancer growth have been demonstrated to be inhibited in cells and animal models by the 13-amino acid peptide SOR-C13 in completed phase I clinical studies. At the moment, there are very few small molecule inhibitors of TRPV6 that have passed clinical trials and are approved drugs [ 77 , 78 , 99 ]. The TRPV6 inhibitors are summarized in Table 1 .…”

Section: Pharmacology Of Trpv6mentioning

confidence: 99%

The TRPV6 Calcium Channel and Its Relationship with Cancer

Wang,

Deng,

Zhang

et al. 2024

Biology

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Transient receptor potential vanilloid-6 (TRPV6) is a cation channel belonging to the TRP superfamily, specifically the vanilloid subfamily, and is the sixth member of this subfamily. Its presence in the body is primarily limited to the skin, ovaries, kidney, testes, and digestive tract epithelium. The body maintains calcium homeostasis using the TRPV6 channel, which has a greater calcium selectivity than the other TRP channels. Several pieces of evidence suggest that it is upregulated in the advanced stages of thyroid, ovarian, breast, colon, and prostate cancers. The function of TRPV6 in regulating calcium signaling in cancer will be covered in this review, along with its potential applications as a cancer treatment target.

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Erratum to: First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors

Cited by 10 publications

References 0 publications

TRPV6 calcium channel directs homeostasis of the mammary epithelial sheets and controls epithelial mesenchymal transition

TRPV6 calcium channel directs homeostasis of the mammary epithelial sheets and controls epithelial mesenchymal transition

TRPV6 as A Target for Cancer Therapy

The TRPV6 Calcium Channel and Its Relationship with Cancer

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