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Updated: Aug 9, 2026
Yeast Luminometric and Xenopus Oocyte Electrophysiological Examinations of the Molecular Mechanosensitivity of TRPV4
Published on: December 31, 2013
Transient receptor potential canonical 4 and 5 proteins as targets in cancer therapeutics
Hannah J Gaunt1, Naveen S Vasudev2, David J Beech3
1School of Medicine, University of Leeds, LIGHT Building, Clarendon Way, Leeds, LS2 9JT, UK. bs10hg@leeds.ac.uk.
Abstract:
Novel approaches towards cancer therapy are urgently needed. One approach might be to target ion channels mediating Ca2+ entry because of the critical roles played by Ca2+ in many cell types, including cancer cells. There are several types of these ion channels, but here we address those formed by assembly of transient receptor potential canonical (TRPC) proteins, particularly those which involve two closely related members of the family: TRPC4 and TRPC5. We focus on these proteins because recent studies point to roles in important aspects of cancer: drug resistance, transmission of drug resistance through extracellular vesicles, tumour vascularisation, and evoked cancer cell death by the TRPC4/5 channel activator (-)-englerin A. We conclude that further research is both justified and necessary before these proteins can be considered as strong targets for anti-cancer cell drug discovery programmes. It is nevertheless already apparent that inhibitors of the channels would be unlikely to cause significant adverse effects, but, rather, have other effects which may be beneficial in the context of cancer and chemotherapy, potentially including suppression of innate fear, visceral pain and pathological cardiac remodelling.
Insights
Targeting TRPC4/5 ion channels offers a novel cancer therapy approach. Inhibitors may suppress pain and cardiac issues, showing potential benefits beyond direct anti-cancer effects.
Area of Science:
- Oncology
- Molecular Biology
- Biophysics
Background:
- Novel cancer therapies are crucial due to increasing drug resistance.
- Calcium (Ca2+) signaling plays a vital role in cancer cell functions.
- Transient Receptor Potential Canonical (TRPC) channels mediate Ca2+ entry and are implicated in cancer.
Purpose of the Study:
- To explore the potential of targeting TRPC4 and TRPC5 ion channels for cancer therapy.
- To review the role of TRPC4/5 channels in cancer drug resistance, vascularization, and cell death.
- To evaluate the therapeutic implications of TRPC4/5 channel activators and inhibitors.
Main Methods:
- Literature review of recent studies on TRPC4/5 channels in cancer.
- Analysis of TRPC4/5 channel involvement in drug resistance and tumor vascularization.
- Examination of cancer cell death induced by TRPC4/5 activators like (-)-englerin A.
Main Results:
- TRPC4/5 channels are involved in cancer drug resistance and its transmission via extracellular vesicles.
- TRPC4/5 channels play a role in tumor vascularization.
- The TRPC4/5 channel activator (-)-englerin A can evoke cancer cell death.
Conclusions:
- TRPC4/5 channels are promising targets for anti-cancer drug discovery.
- Inhibitors of TRPC4/5 channels may offer benefits beyond direct anti-cancer effects, including pain and cardiac remodeling suppression.
- Further research is necessary to fully establish TRPC4/5 channels as therapeutic targets.
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