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Significance Filarial nematodes affect millions of people globally and constitute a serious public health issue in tropical and subtropical regions. Ivermectin (IVM) is used in combination with other chemotherapeutic agents… Click to show full abstract
Significance Filarial nematodes affect millions of people globally and constitute a serious public health issue in tropical and subtropical regions. Ivermectin (IVM) is used in combination with other chemotherapeutic agents for treatment and control of filarial infections. Glutamate-gated chloride channels (GluCls) are targeted by IVM to produce hyperpolarization and muscle paralysis. This is effective in clearing microfilariae from the host and suppresses their reappearance but has limited adulticidal activity. Here, we functionally expressed and characterized a Brugia malayi AVR-14B GluCl channel, investigated the physiological relevance, and elucidated the pharmacological spectrum of the receptor to establish its validity as a drug target. We used electrophysiology and pharmacology to gain a mechanistic understanding of IVM and nodulisporic acid (NA) activity on the channel.
Journal Title: Proceedings of the National Academy of Sciences of the United States of America
Year Published: 2022
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