Target intelligence / Profile preview

Sodium- and chloride-dependent glycine transporter 1 (GlyT1)

Target
GlyT1
Molecular classification
Transporter, Solute carrier family, Sodium:neurotransmitter symporter
01

Overview

Sodium- and chloride-dependent glycine transporter 1 (GlyT1) is a transmembrane protein encoded by the SLC6A9 gene and predominantly expressed in glial cells and at glutamatergic synapses in the central nervous system[6][5][7]. GlyT1 is essential for tightly regulating extracellular glycine concentrations at inhibitory glycinergic synapses and for modulating NMDA receptor activation, where glycine acts as a necessary co-agonist[5][1]. By controlling synaptic glycine, GlyT1 modulates glutamatergic neurotransmission and influences cognitive functions. Dysregulation or mutation of GlyT1 can result in neurological disorders such as glycine encephalopathy[6]. GlyT1 inhibitors, such as bitopertin and iclepertin, have been clinically explored to enhance cognitive function in schizophrenia and related disorders by increasing glycine levels and thereby strengthening NMDA receptor-mediated neurotransmission[6][4].

Other names
Glycine transporter 1GlyT-1SLC6A9
02

Mechanism of action

Inhibition increases synaptic glycine levels and potentiates NMDA receptor function, Enhancement of cognitive function via NMDA receptor modulation

03

Biological functions

Regulation of glycine concentrationRegulation of NMDA receptor functionSynaptic transmissionNeurotransmitter reuptake
04

Disease associations

SchizophreniaCognitive disordersGlycine encephalopathyNeurodegenerative diseaseMuscle tone disorderEpilepsyPain
05

Safety considerations

Risk of excessive NMDA activationPotential CNS side effectsMetabolic disorders such as glycine encephalopathy with normal serum glycine
06

Interacting drugs

Bitopertin

6 more in the full profile.

07

Biomarkers

Mutations (e.g., for glycine encephalopathy)SLC6A9 gene status

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