Definition Members of the Cys-loop receptor class are ligand-gated ion channels that open in response to binding of ACh, 5-HT (serotonin), Glycine, GABA . Cys loop receptor channels form from homo- or hetero-tetrameric arrangement of subunits surrounding an aqueous pore. Each subunit consists...
This Cys-loop structure is important in the intersubunit assembly because blocking its formation negatively affects the receptor assembly (Green & Wanamaker, 1997). The N-terminal domains of the five subunits form the ligand-binding domain, which lies in the interfaces of adjacent subunits. The ...
Because operating on individual biogenesis steps influences the receptor cell surface level, manipulating the proteostasis network components can regulate the function of the receptors, representing an emerging therapeutic strategy for corresponding channelopathies.Yan-Lin Fu *...
The Cys-loop receptor superfamily of ligand-gated ion channels has a prominent role in neuronal signalling. These receptors are pentamers, each subunit containing ten β-strands in the extracellular domain and four α-helical transmembrane domains (M1–M4). The M2 domain of each subunit lines ...
To ensure that the mutations did not adversely perturb the general structure, function or long-term trafficking of the receptor, we monitored both the dose–response curves and the recovery phase of the currents from desensitiza- tion for selected mutants. Overall, the concentration–response ...
Structure of a key eukaryotic Cys-loop receptor The atomic resolution structure of the glutamate-gated chloride channel (GluCl) fromCaenorhabditis eleganshas been determined, in the presence of the allosteric agonist ivermectin, the endogenous neurotransmitter L-glutamate and the open-channel blocker picr...
Until recently, the binding site on its Cys-loop receptor target had been a mystery. Recent protein crystal structures, site-directed mutagenesis data and molecular modelling now explain how ivermectin binds to these receptors and reveal why it is selective for invertebrate members of the Cys-loop...
[63], the cys-loop LGIC superfamily has remained compact with only minor changes in gene numbers. However, alternative splicing and RNA A-to-I editing have considerably increased receptor diversity, effectively introducing changes in functionally significant and highly conserved regions to generate ...
The 5-HT3 receptor is a member of the Cys-loop family of ligand-gated ion channels. These receptors are located in both the peripheral and central nervous systems, where functional receptors are constructed from five subunits. These subunits may be the same (homopentameric 5-HT3A receptors) ...
To investigate receptor-agonist interactions, alterations in the structure of the agonist or receptor may be introduced. Here we manipulate the structure of the ligand while observing the binding and functional properties of a series of bischoline agonists at recombinant Torpedo nAChRs expressed in ...