The superfamily of pentameric ion channel neurotransmitter receptors has undergone a dramatic expansion with the discovery that invertebrates encode a vastly larger and more diverse complement of receptor subunits than are found in vertebrates. Where vertebrates have excitatory acetylcholine and inhibitory GABA and glycine receptors, invertebrates encode, in addition, inhibitory glutamate, acetylcholine, serotonin and tyramine receptors as well as excitatory GABA and proton-gated receptors. This receptor diversity appears to be quite ancient, predating the vertebrate-invertebrate split. The diversity of invertebrate channels is also the Achilles heel of invertebrate parasites and pests. Of the five successful antiparasitic nematocides, three act on invertebrate neurotransmitter receptors. We are currently validating orphan receptors from the nematode C. elegans and the fruit fly Drosophila as targets for novel antiparasitics and pesticides respectively. We propose that a directed approach to drug discovery based on characterized targets can lead to safer, more efficacious antiparasitics and pesticides.


Seminar, October 24, 2013, 12:30. Seminar Room

Hosted by Melike Lakadamyali