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GABAA receptor family: overview on structural characterization
(Future Science, 2019-02-25)
The pentameric γ-aminobutyric acid type A receptors are ion channels activated by ligands, which intervene in the rapid inhibitory transmission in the mammalian CNS. Due to their rich pharmacology and therapeutic potential, ...
A Latin American perspective on ion channels
(American Society for Pharmacology and Experimental Therapeutics, 2016-09)
Ion channels, both ligand- And voltage-gated, play fundamental roles in many physiologic processes. Alteration in ion channel function underlies numerous pathologies, including hypertension, diabetes, chronic pain, epilepsy, ...
Structure and function development during evolution of pentameric ligand gated ion channels
(Smart Science and Technology, 2016-01)
Ligand Gated Ion Channels (LGICs) are receptors widely involved in vertebrate neuronal and non-neuronal signalling as well as muscle activation. Until very recently these receptors, were only known to exist in animal cells ...
A structural view of ligand-dependent activation in thermoTRP channels
(Frontiers Research Foundation, 2014)
Transient Receptor Potential (TRP) proteins are a large family of ion channels, grouped into seven sub-families. Although great advances have been made regarding the activation and modulation of TRP channel activity, ...
Design, synthesis and functional evaluation of a novel series of phosphonate-functionalized 1,2,3-triazoles as positive allosteric modulators of α7 nicotinic acetylcholine receptors
(American Chemical Society, 2020-07-28)
The α7 nicotinic acetylcholine receptor is a pentameric ligand-gated ion channel widely distributed in the central nervous system, mainly in hippocampus and cortex. The enhancement of its activity by positive allosteric ...
Nicotinic acetylcholine receptors at the single-channel level
(Wiley Blackwell Publishing, Inc, 2018-06)
Over the past four decades, the patch clamp technique and nicotinic ACh (nACh) receptors have established an enduring partnership. Like all good partnerships, each partner has proven significant in its own right, while ...
MUTAGENESIS AND TEMPERATURE-SENSITIVE LITTLE MACHINES
(INTECH, 2012)
In mammals a class of ion channels able to sense a wide range of temperatures (0-60 °C) has evolved. These molecular thermodynamic machines called thermo Transient Receptor Potential (thermoTRP) are spread through the ...
Conserved patterns across ion channels correlate with variant pathogenicity and clinical phenotypes
(2022)
Clinically identified genetic variants in ion channels can be benign or cause disease by increasing or decreasing the protein function. As a consequence, therapeutic decision-making is challenging without molecular testing ...
Role of the cys loop and transmembrane domain in the allosteric modulation of α4β2 nicotinic acetylcholine receptors
(American Society for Biochemistry and Molecular Biology Inc., 2017)
© 2017 by The American Society for Biochemistry and Molecular Biology, Inc.Allosteric modulators of pentameric ligand-gated ion channels are thought to act on elements of the pathways that couple agonist binding to channel ...