Structural Properties, Pathophysiological Relevance and Synthetic Modulators of TRPC Channels
Xue Qiao1,2,3, Chunlin Ren1,2,4,5, Wumei Wang3,5
1Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery Yantai, Shandong, China.
Medicinal Research Reviews
|July 30, 2025
Summary
Transient receptor potential canonical (TRPC) channels are key in health and disease. New structural insights and selective drugs offer therapeutic potential for TRPC-related conditions.
Area of Science:
- Molecular Biology
- Pharmacology
- Structural Biology
Background:
- Transient receptor potential canonical (TRPC) channels are calcium-permeable cation channels regulating vital physiological functions.
- Dysregulation of TRPC channels is linked to neurological, cardiovascular, and chronic kidney diseases.
- TRPC channels represent a promising therapeutic target for various pathologies.
Purpose of the Study:
- To review the structural and functional characteristics of TRPC channels.
- To explore the role of TRPC channels in physiological processes and disease states.
- To guide the development of TRPC-targeted therapeutics by integrating structural biology and medicinal chemistry.
Main Methods:
- Cryo-electron microscopy (cryo-EM) for structural elucidation of TRPC channels.
- Development and application of subtype-selective TRPC modulators.
- Analysis of structure-activity relationships for drug discovery.
Main Results:
- Recent cryo-EM studies have revealed detailed TRPC channel structures.
- Subtype-selective modulators have provided insights into TRPC channel functions in pathophysiology.
- Several TRPC-targeting compounds demonstrate preclinical efficacy.
Conclusions:
- Understanding TRPC channel structure and function is crucial for disease intervention.
- Medicinal chemistry efforts are yielding promising selective TRPC modulators.
- This review offers strategic direction for developing clinically applicable TRPC therapeutics.
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