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Review
. 2022 Dec 4;23(23):15289.
doi: 10.3390/ijms232315289.

Thermo-Transient Receptor Potential Channels: Therapeutic Potential in Gastric Cancer

Gang-Fan Zong  1 , Rui Deng  1 , Su-Yun Yu  1   2 , Ai-Yun Wang  1   3 , Zhong-Hong Wei  1 , Yang Zhao  2 , Yin Lu  1   3
Affiliations
Review

Thermo-Transient Receptor Potential Channels: Therapeutic Potential in Gastric Cancer

Gang-Fan Zong et al. Int J Mol Sci. .

Abstract

Over the last decade, researchers have found abnormal expression of transient receptor potential (TRP) channels. In particular, members of the thermally sensitive subclass (thermo-TRPs) are involved in many disease processes. Moreover, they have a vital role in the occurrence and development of gastric cancer (GC). Accordingly, thermo-TRPs constitute a major pharmacological target, and the elucidation of the mechanisms underlying their response to physiological stimuli or drugs is key for notable advances in GC treatment. Therefore, this paper summarizes the existing literature about thermo-TRP protein expression changes that are linked to the incidence and progression of GC. The review also discusses the implication of such association to pathology and cell physiology and identifies potential thermo-TRP protein targets for diagnosis and treatment of GC.

Keywords: TRP; gastric cancer; ion channel; temperature; therapeutic target.

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Conflict of interest statement

The authors declare that they have no conflict of interest.

Figures

Figure 1
Figure 1
The activation of thermo-TRPs by specified temperature and particular compounds. Thermo-TRPs are expressed in diverse cell lines and are activated by ambient changes. TRPA1 is activated by noxious cold (≤17 °C). TRPM8, TRPM5, TRPC5, TRPV4, TRPM3, and TRPM2 are activated by innocuous warm and cool stimuli (ranges from 15–35 °C). Whereas TRPM4, TRPV1, and TRPV2 are activated by heat in the noxious range, with respective thresholds of 40 °C, 42 °C, and 52 °C. Moreover, all thermo-TRPs can also be activated by various agonists present in the environment. Thermo-TRPs, thermo-sensitive transient receptor potential channels.
Figure 2
Figure 2
The TRP channels are composed of six transmembrane-spanning domains (S1–S6) that have a pore-forming loop connecting S5 and S6 as well as N and C termini situated intracellularly. In the S6 region, there are some structural differences between thermo-TRPs.
Figure 3
Figure 3
Representative agonist and antagonist structures of thermo-TRPs are approved by the FDA. In Figure 3, the agonists of thermo-TRPs are on the left in the red background, and the antagonists of thermo-TRPs are on the right in the blue background.
Figure 4
Figure 4
Mechanism of gastric cancer proliferation, invasion and metastasis mediated by representative thermo-TRPs.
See this image and copyright information in PMC

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