Advances in the Study for Modulators of Transient Receptor Potential Vanilloid (TRPV) Channel Family.

Curr Top Med Chem

School of Pharmacy & School of Biological and Food Engineering, Changzhou University, Changzhou, 213164, Jiangsu, PR China.

Published: January 2025

AI Article Synopsis

  • TRPV channels are part of a larger superfamily and are found in many cell types, with TRPV1-4 being sensitive to temperature and TRPV5-6 being selective for calcium ions.
  • These channels are important in various physiological processes and can be influenced by internal and external compounds, making them a target for pharmacological research.
  • Modulating these channels is crucial because it could lead to treatments for diseases like neurodegenerative disorders, pain, cancer, and skin issues, and there has been recent progress in exploring their ligands and related pharmacological effects.

Article Abstract

Transient receptor potential vanilloid (TRPV) channels are a member of the TRP superfamily, which consists of six proteins and is expressed in many neuronal and non-neuronal cells. Among them, TRPV1-4 are non-selective cation channels that are highly sensitive to temperature changes, while TRPV5-6 are channels that are highly selective to Ca2+. These cation channels have attracted great interest academically, especially from a pharmacological perspective. TRPV channels play a vital role in many physiological processes and can be regulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. The regulation of their activities can lead to a variety of diseases and disorders, such as neurodegenerative diseases, pain, cancer, and skin diseases. In fact, several TRPV1 and TRPV3 modulators have been developed for clinical use. Therefore, the development of TRPV channel modulators has important clinical significance and value. Herein, we focused on and summarized the latest research progress of endogenous and exogenous ligands of six TRPV channels and their pharmacological effects on related diseases.

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http://dx.doi.org/10.2174/0115680266294569241115053420DOI Listing

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Article Synopsis
  • TRPV channels are part of a larger superfamily and are found in many cell types, with TRPV1-4 being sensitive to temperature and TRPV5-6 being selective for calcium ions.
  • These channels are important in various physiological processes and can be influenced by internal and external compounds, making them a target for pharmacological research.
  • Modulating these channels is crucial because it could lead to treatments for diseases like neurodegenerative disorders, pain, cancer, and skin issues, and there has been recent progress in exploring their ligands and related pharmacological effects.
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