Know more

Macrocyclic lactones are the most widely used anthelmintic drugs for the treatment of parasitic nematodes both in human and animal health. They are agonists of the nematode glutamate-gated chloride channels (GluCls). GluCls subunit composition and pharmacological properties remain largely unknown in most nematodes. A research team at INRAE Nouzilly looked into GluCl diversity and mode of action of macrocyclic lactones and identified and pharmacologically characterised receptors made of highly conserved GluCl subunits. They reconstituted a total of 14 GluCls and observed that the GLC-2 subunit plays a pivotal role in the composition of heteromeric GluCls in nematodes. They also identified a novel GluCl subtype for which a high concentration of the anthelmintics ivermectin and moxidectin reversibly potentiates glutamateinduced response. The study brings a new vision to the diversity of GluCl subtypes in nematodes and promotes novel drug targets for next generation of anthelmintic compounds development.

Link : https://pubmed.ncbi.nlm.nih.gov/34623639/

Authors : Lamassiaude N, Courtot E, Corset A, Charvet CL, Neveu C

DOI : 10.1111/bph.15703