Transient receptor potential canonical (TRPC) channels

TRPC channels constitute a group of receptor-operated Ca²⁺-permeable nonselective cation channels of the TRP superfamily. Seven mammalian TRPC channel proteins (TRPC1-7) have been identified, and divided into four subgroups (TRPC1, TRPC2, TRPC4/5, and TRPC3/6/7), which can form homomeric or heteromeric channels. TRPC1 is highly expressed in different tissues. TRPC2 is a pseudogene in humans. TRPC3 expression is high in the brain, especially in pituitary gland and Purkinje cells of the cerebellum. TRPC4 is highly expressed in the cortico-limbic regions of the brain and in dopaminergic neurons. TRPC5 is also expressed in brain tissues, but it also has a key role in sensing pressure at the aortic baroreceptors, and in chemotherapy-induced multidrug resistance by promoting expression of p-glycoprotein and ABCB1 in cancer cells. TRPC6 is widely expressed in internal organs and in the brain. TRPC7 is expressed in human kidneys, pituitary gland, and brain. Expression patterns may be different in mammalian species.

The activity of TRPC channels is largely regulated by their interaction with a variety of receptors. Diacylglycerols (DAGs) can directly activate mammalian TRPC channels. Intra- or extracellular [Ca²⁺] can activate or inhibit the TRPC channels. Several drugs can directly interact with TRPC channels.

[¹¹C]HC070 is a TRPC5-specific radiotracer that has shown promising results in preclinical studies (Yu et al., 2023).

See also:

• Voltage-gated sodium channels

---

Literature

Wang H, Cheng X, Tian J, Xiao Y, Tian T, Xu F, Hong X, Zhu MX. TRPC channels: Structure, function, regulation and recent advances in small molecular probes. Pharmacol Ther. 2020; 209: 107497. doi: 10.1016/j.pharmthera.2020.107497.

Tags: (none)

---

Updated at: 2023-08-02
Created at: 2023-08-02
Written by: Vesa Oikonen