TRPA1
Författare
Redaktör
- Bernd Nilius
- Veit Flockerzi
Summary, in English
The transient receptor potential ankyrin subtype 1 protein (TRPA1) is a nonselective cation channel permeable to Ca(2+), Na(+), and K(+). TRPA1 is a promiscuous chemical nocisensor that is also involved in noxious cold and mechanical sensation. It is present in a subpopulation of Aδ- and C-fiber nociceptive sensory neurons as well as in other sensory cells including epithelial cells. In primary sensory neurons, Ca(2+) and Na(+) flowing through TRPA1 into the cell cause membrane depolarization, action potential discharge, and neurotransmitter release both at peripheral and central neural projections. In addition to being activated by cysteine and lysine reactive electrophiles and oxidants, TRPA1 is indirectly activated by pro-inflammatory agents via the phospholipase C signaling pathway, in which cytosolic Ca(2+) is an important regulator of channel gating. The finding that non-electrophilic compounds, including menthol and cannabinoids, activate TRPA1 may provide templates for the design of non-tissue damaging activators to fine-tune the activity of TRPA1 and raises the possibility that endogenous ligands sharing binding sites with such non-electrophiles exist and regulate TRPA1 channel activity. TRPA1 is promising as a drug target for novel treatments of pain, itch, and sensory hyperreactivity in visceral organs including the airways, bladder, and gastrointestinal tract.
Avdelning/ar
Publiceringsår
2014
Språk
Engelska
Sidor
583-630
Publikation/Tidskrift/Serie
Mammalian Transient Receptor Potential (TRP) Cation Channels: Handbook of Experimental Pharmacology
Volym
I
Länkar
Dokumenttyp
Del av eller Kapitel i bok
Ämne
- Medicinal Chemistry
- Pharmacology and Toxicology
Status
Published
ISBN/ISSN/Övrigt
- ISBN: 9783642542152