Results 221 to 230 of about 8,825 (235)

Towards a KCC2 blocker pharmacophore model

Bioorganic & Medicinal Chemistry Letters, 2012
A multi-disciplinary approach was used to identify the first pharmacophore model for KCC2 blockers: several physico-chemical studies such as XRD and NMR were combined to molecular modelling techniques, SAR analysis and synthesis of constrained analogues in order to determine a minimal conformational space regrouping few potential bioactive ...
Florence, Lebon, Cécile, Pégurier, Marie, Ledecq, Benoit, Mathieu, Nathalie, Bosman, Anne, Frycia, Sébastien, Lengelé, Kashinath, Dhurke, Ananda Kumar, Kanduluru, Stéphane, Meunier, Alain, Wagner, Christian, Wolff, Laurent, Provins   +12 more
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Behavioural phenotypes of hypomorphic KCC2‐deficient mice

European Journal of Neuroscience, 2005
AbstractHyperpolarizing fast inhibitory neurotransmission by γ‐aminobutyric acid and glycine requires an efficient chloride extrusion mechanism in postsynaptic neurons. A major effector of this task in adult animals is the potassium‐chloride co‐transporter KCC2 that is selectively and abundantly expressed postsynaptically in most CNS neurons.
Janne, Tornberg, Vootele, Voikar, Harri, Savilahti, Heikki, Rauvala, Matti S, Airaksinen   +4 more
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Neuronal Restrictive Silencing Element Is Found in the KCC2 Gene: Molecular Basis for KCC2-Specific Expression in Neurons

Journal of Neurophysiology, 2001
KCC2 is one of four known isoforms of the K-Cl cotransporter with an expression pattern restricted to neurons. It mediates efflux of Cl− across neuronal membranes and plays an important role in GABAergic and glycinergic neurotransmission. To understand the molecular basis for neuronal specificity of KCC2 expression, we isolated and sequenced portions ...
M F, Karadsheh, E, Delpire
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The KCC2 Cotransporter and Human Epilepsy

The Neuroscientist, 2016
The cation-Cl− cotransporter KCC2, encoded by SLC12A5, is required for the emergence and maintenance of GABAergic fast synaptic inhibition in organisms across evolution. These findings have suggested that KCC2 deficiency might play a role in the pathogenesis human epilepsy, but this has only recently been substantiated by two lines of genetic evidence.
Kristopher T, Kahle, Arjun R, Khanna, JingJing, Duan, Kevin J, Staley, Eric, Delpire, Annapurna, Poduri   +5 more
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Benzyl prolinate derivatives as novel selective KCC2 blockers

Bioorganic & Medicinal Chemistry Letters, 2010
The discovery and optimization of a novel class of selective submicromolar KCC2 blockers is described. Details of synthesis and SAR are given together with ADME properties of selected compounds. A methylsulfone residue on the R(1) phenyl group improved the overall general profile of these prolinate derivatives.
Cécile, Pégurier, Nathalie, Bosman, Philippe, Collart, Marie-Laure, Delporte, Karine, Leclercq, Sébastien, Lengelé, Ananda Kumar, Kanduluru, Stéphane, Meunier, Nathalie, Pacico, Lakshmana Rao, Vadali, Alain, Wagner, Christian, Wolff, Laurent, Provins   +12 more
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Distribution and Cellular Localization of KCC2 in the Ferret Neocortex

Developmental Neuroscience, 2018
KCC2 (a brain-specific potassium-chloride cotransporter) affects development of the cerebral cortex, including aspects of neuronal migration and cellular maturation and differentiation. KCC2 also modulates chloride homeostasis by influencing the switch of GABA from depolarizing in young neurons to hyperpolarizing in mature neurons.
Francis T, Djankpa, Oluwole B, Akinola, Sharon L, Juliano   +2 more
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Role of KCC2 in Auditory Processing of the Brainstem

2006
The present study indicates that the neuro-specific co-transporter KCC2 is expressed abundantly throughout the IC. The postnatal expression pattern of KCC2 is upregulated in the IC as well as that in the neocortex, the hippocampus and the cerebellum. Considering the importance of this co-transporter on controlling auditory function, further studies are
Motoi Kudo, Takaaki Nakamura, Kiyoshi Kurokawa   +2 more
openaire   +1 more source

Genetic and environmental regulators of Kcc2/KCC2 gene expression

2020
Michele Yeo, Wolfgang Liedtke
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KCC2 regulates dendritic spine development

2020
Olaya Llano, Claudio Rivera, Anastasia Ludwig   +2 more
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Intracellular taurine inhibits KCC2 transporter activity

Neuroscience Research, 2010
Koichi Inoue, Tomonori Furukawa, Tatsuro Kumada, Junko Jamada, Tianying Wang, Atsuo Fukuda   +5 more
openaire   +1 more source