Cadmium opens GluK2 kainate receptors with cysteine substitutions at the M3 helix bundle crossing.

ABSTRACT: Kainate receptors are ligand-gated ion channels that have two major roles in the central nervous system: they mediate a postsynaptic component of excitatory neurotransmission at some glutamatergic synapses and modulate transmitter release at both excitatory and inhibitory synapses. Accumulating evidence implicates kainate receptors in a variety of neuropathologies, including epilepsy, psychiatric disorders, developmental delay, and cognitive impairment. Here, to gain a deeper understanding of the conformational changes associated with agonist binding and channel opening, we generate a series of Cys substitutions in the GluK2 kainate receptor subunit, focusing on the M3 helices that line the ion pore and form the bundle-crossing gate at the extracellular mouth of the channel. Exposure to 50

SUBMITTER: Wilding TJ 

PROVIDER: S-EPMC6445585 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature