Article
Molecular mechanism of setron-mediated inhibition of full-length 5-HT3A receptor.
Nature communications - 19 Jul 2019
Basak Sandip, Gicheru Yvonne, Kapoor Abhijeet, Mayer Megan L, Filizola Marta, Chakrapani Sudha
Abstract excerpt
Serotonin receptor (5-HT3AR) is the most common therapeutic target to manage the nausea and vomiting during cancer therapies and in the treatment of irritable bowel syndrome. Setrons, a class of competitive antagonists, cause functional inhibition of 5-HT3AR in the gastrointestinal tract and brainstem, acting as effective anti-emetic agents. Despite their prevalent use, the molecular mechanisms underlying setron...
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