Neuronal K+-Cl- cotransporter KCC2 as a promising drug target …
WEBSep 13, 2023 · The neuron-specific K + -Cl - cotransporter 2 (KCC2) is essential for maintaining a low intracellular Cl - concentration, ensuring GABA A R-mediated inhibition. Impaired KCC2 function results...
The Expanding Therapeutic Potential of Neuronal KCC2 - PMC
WEBJan 17, 2020 · The potassium–chloride cotransporter 2 (KCC2, SLC12A5) is a key modulator of inhibitory GABAergic inputs in healthy adult neurons, as its chloride (Cl −) extruding activity underlies the hyperpolarizing reversal potential for GABA A receptor Cl − currents (E GABA ).
The Therapeutic Potential of Neuronal K-Cl Co-Transporter KCC2 …
WEBNov 30, 2020 · Intracellular chloride levels in the brain are regulated primarily through the opposing effects of two cation-chloride co-transporters (CCCs), namely K + -Cl − co-transporter-2 (KCC2) and Na + -K + -Cl − co-transporter-1 (NKCC1).
Molecular architecture of potassium chloride co-transporter KCC2
WEBNov 28, 2017 · KCC2 is a neuron specific K + -Cl − co-transporter that controls neuronal chloride homeostasis, and is critically involved in many neurological diseases including brain trauma,...
Targeting ischemia-induced KCC2 hypofunction rescues …
WEBNov 9, 2021 · In a CD-1 mouse model of refractory ischemic neonatal seizures, treatment with the KCC2 functional enhancer CLP290 rescued phenobarbital efficacy, increased KCC2 abundance, and prevented the development of epileptogenesis, as quantified by video electroencephalogram monitoring.
The structural basis of function and regulation of neuronal ...
WEBFeb 17, 2021 · Cation-chloride cotransporters (CCC) are central to the regulation of intracellular Cl − concentration and have key physiological roles in neuronal excitability, trans-epithelial salt and...
Small-molecule screen identifies inhibitors of the neuronal K-Cl ...
WEBMar 31, 2009 · KCC2, a neuronal-specific K-Cl cotransporter, plays a major role in maintaining intracellular Cl(-) concentration in neurons below its electrochemical equilibrium potential, thus favoring robust GABA hyperpolarizing or inhibitory responses.
Preclinical insights into therapeutic targeting of KCC2 for
WEBTo that end, targeting the electroneutral K + /Cl - cotransporter KCC2 has emerged as a novel therapeutic strategy for the treatment of epilepsy. Areas covered: We summarize the roles of KCC2 in the maintenance of synaptic inhibition and the evidence linking KCC2 dysfunction to epileptogenesis.
Neuronal K+-Cl- cotransporter KCC2 as a promising drug target …
WEBSep 13, 2023 · The neuron-specific K +-Cl-cotransporter 2 (KCC2) is essential for maintaining a low intracellular Cl-concentration, ensuring GABA A R-mediated inhibition. Impaired KCC2 function results in GABAergic excitation associated with epileptic activity.
The Neuron-specific K-Cl Cotransporter, KCC2 - Journal of …
WEBThe neuron-specific K-Cl cotransporter (KCC2) is hypothesized to function as an active Cl − extrusion pathway important in postsynaptic inhibition mediated by ligand-gated anion channels, like γ-aminobutyric acid type A (GABA A) and glycine receptors.
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