Transient receptor potential (TRP) channels are a group of ion channels located mostly on the plasma membrane of different cell types. In mammals, TRP channels comprise 28 members and based on the homology of amino acid sequences, they are divided into six subfamilies: TRPC (Canonical), TRPV (Vanilloid), TRPM (Melastatin), TRPP (Polycystin), TRPML (Mucolipin), and TRPA (Ankyrin). TRP ion channels are widely expressed in many different tissues and cell types. They can function as cellular sensors involved in nociception, taste perception, thermosensation, and osmolarity sensing. Besides, they also play a critical role in other physiological processes like signal transmission and ion homeostasis. Dysfunction of TRP channels can cause several inherited diseases in humans that affect the cardiovascular, renal, skeletal and nervous systems. Moreover, they are regarded as promising targets for drug discovery.
The TRPC subfamily consists of several isoforms, which are nonselective cation channels. They have a broad tissue distribution in both central nervous system and peripheral tissues. Now, these channels have gained interest as potential therapeutic targets for a variety of diseases, including respiratory diseases, neurological disorders, cardiovascular disorders, pain, cancer, etc. Small molecule inhibitors or modulators are being developed by pharmaceutical companies and academic institutes. Here, we give an introduction to the properties, functions, drug discovery of the following human TRPC channels.
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