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  • The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand.

The anthelmintic praziquantel is a human serotoninergic G-protein-coupled receptor ligand.

Nature communications (2017-12-07)
John D Chan, Pauline M Cupit, Gihan S Gunaratne, John D McCorvy, Yang Yang, Kristen Stoltz, Thomas R Webb, Peter I Dosa, Bryan L Roth, Ruben Abagyan, Charles Cunningham, Jonathan S Marchant
ABSTRACT

Schistosomiasis is a debilitating tropical disease caused by infection with parasitic blood flukes. Approximately 260 million people are infected worldwide, underscoring the clinical and socioeconomic impact of this chronic infection. Schistosomiasis is treated with the drug praziquantel (PZQ), which has proved the therapeutic mainstay for over three decades of clinical use. However, the molecular target(s) of PZQ remain undefined. Here we identify a molecular target for the antischistosomal eutomer - (R)-PZQ - which functions as a partial agonist of the human serotoninergic 5HT