Andreas Jurik

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Nerve functions require phosphatidylinositol-4,5-bisphosphate (PIP2) that binds to ion channels, thereby controlling their gating. Channel properties are also attributed to serotonin transporters (SERTs); however, SERT regulation by PIP2 has not been reported. SERTs control neurotransmission by removing serotonin from the extracellular space. An increase in(More)
Elevating GABA levels in the synaptic cleft by inhibiting its reuptake carrier GAT1 is an established approach for the treatment of CNS disorders like epilepsy. With the increasing availability of crystal structures of transmembrane transporters, structure-based approaches to elucidate the molecular basis of ligand-transporter interaction also become(More)
Tiagabine (Gabitril ®) is a selective inhibitor of the human gamma-aminobutyric acid (GABA) transporter 1 (hGAT-1), a transport protein belonging to the family of neurotransmitter-sodium-symporters (NSS). It is a marketed drug, used for treatment of epilepsy. However, the molecular basis of protein-ligand interaction remains obscure due to the lack of a 3D(More)
Termination of GABA-ergic signaling requires fast uptake of the neurotransmitter by highly selective transporter proteins. Four subtypes of sodium-and chloride-dependent GABA transporters exist, GAT-1 being the most prominent one in the brain. The only marketed drug targeting this transporter system is the anticonvulsant tiagabine. [1] It is highly GAT-1(More)
The human transporters for the inhibitory neurotrans-mitter gamma-aminobutyric acid (GABA) hGAT-1, 2, and 3, and hBGT-1 belong to the neurotransmitter-sodium symporter (NSS) family of membrane transport proteins. hGAT-1 has been a target for the design of antiepileptic therapeutics [1], with tiagabine (Gabitril ®) being the only GAT inhibitor on the market.(More)
  • Florian Buchmayer, Klaus Schicker, Gerald Stübiger, Peter J Hamilton, Petra Geier, Andreas Jurik +12 others
  • 2011
Background Neuronal functions, such as excitability or endo-and exo-cytosis, require phosphatidylinositol-4,5-bisphosphate (PIP 2) since ion channels and other proteins involved in these processes are regulated by PIP 2. Monoamine transporters control neurotransmission by removing monoa-mines from the extracellular space. They also display channel(More)
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