Coumarins as TRPA1 Antagonists
In the year 2014 the PI interested in Transient Receptor Potential Ankyrin 1 (TRPA1), a Ca2+-ion chanel believed to be responsible for noxious pain sensation. It is activated and antagonized by mani natural compounds, and one interesting group of antagonists are stilbenes. TRPA1 is also believed to be a potential target for medication of neuropathic pain. TRPA1 is also strongly connected to inflammation, which makes it even more interesting drug target.
Our collaboration with the Immunopharmacology research group (School of Medicine, The University of Tampere) and the Sirtuin research group (School of Pharmacy, Unierrsity of Eastern Finalnd) has shown a number of coumarin derivatives as highly potential antagonists for TRPA1. We have also found a potential binding pocket for known antagonists resveratrol and pinosylvin as well as several substituted 3-phenyl coumarins. These results were published in ACS Letter in Medicinal chemistry (2024)[1]
[1] Sallomy et al. (2024) ACS Med. Chem. Lett. 15(8): 1221-1226.