Recent progress in the discovery of non-sarcosine based GlyT1 inhibitors

SE Wolkenberg, C Sur - Current topics in medicinal chemistry, 2010 - ingentaconnect.com
The simple amino acid glycine is implicated in both inhibitory and excitatory
neurotransmission in mammalian central nervous system, and it modulates excitatory …

Functional expression of release-regulating glycine transporters GLYT1 on GABAergic neurons and GLYT2 on astrocytes in mouse spinal cord

L Raiteri, S Stigliani, C Usai, A Diaspro… - Neurochemistry …, 2008 - Elsevier
It is widely accepted that glycine transporters of the GLYT1 type are situated on astrocytes
whereas GLYT2 are present on glycinergic neuronal terminals where they mediate glycine …

Glycine transporter 1 inhibitors and modulation of NMDA receptor-mediated excitatory neurotransmission

C Sur, GG Kinney - Current drug targets, 2007 - ingentaconnect.com
In the central nervous system, glutamate is essential for a proper synaptic communication in
neuronal networks supporting critical behavioral activities such as learning and memory …

Zn2+ inhibits glycine transport by glycine transporter subtype 1b

P Ju, KR Aubrey, RJ Vandenberg - Journal of Biological Chemistry, 2004 - ASBMB
In the central nervous system, glycine is a co-agonist with glutamate at the N-methyl-d-
aspartate subtype of glutamate receptors and also an agonist at inhibitory, strychnine …

Transport mechanism and pharmacology of the human GlyT1

Y Wei, R Li, Y Meng, T Hu, J Zhao, Y Gao, Q Bai, N Li… - Cell, 2024 - cell.com
Summary The glycine transporter 1 (GlyT1) plays a crucial role in the regulation of both
inhibitory and excitatory neurotransmission by removing glycine from the synaptic cleft …

Glycine transporter 1 is a target for the treatment of epilepsy

HY Shen, EA Van Vliet, KA Bright, M Hanthorn… - …, 2015 - Elsevier
Glycine is the major inhibitory neurotransmitter in brainstem and spinal cord, whereas in
hippocampus glycine exerts dual modulatory roles on strychnine-sensitive glycine receptors …

Constitutive endocytosis and turnover of the neuronal glycine transporter GlyT2 is dependent on ubiquitination of a C-terminal lysine cluster

J de Juan-Sanz, E Núñez, B López-Corcuera… - PLoS …, 2013 - journals.plos.org
Inhibitory glycinergic neurotransmission is terminated by sodium and chloride-dependent
plasma membrane glycine transporters (GlyTs). The mainly glial glycine transporter GlyT1 is …

[HTML][HTML] Cloning and expression of a spinal cord-and brain-specific glycine transporter with novel structural features.

QR Liu, B Lopez-Corcuera, S Mandiyan… - Journal of Biological …, 1993 - Elsevier
A novel glycine transporter (GLYT2) was cloned from a rat brain cDNA library. GLYT2 is
about 48 and 50% homologous to the previously cloned mouse glycine transporter (GLYT1) …

Analysis of a gene encoding two glycine transporter variants reveals alternative promoter usage and a novel gene structure

B Borowsky, BJ Hoffman - Journal of Biological Chemistry, 1998 - ASBMB
The rat GLYT-1 gene encodes two glycine transporter variants, GLYT-1a and GLYT-1b, that
differ in NH 2 termini and 5′-noncoding regions as well as in tissue distribution. The GLYT …

Transmembrane domain III plays an important role in ion binding and permeation in the glycine transporter GLYT2

J Ponce, B Biton, J Benavides, P Avenet… - Journal of Biological …, 2000 - ASBMB
The neuronal glycine transporter GLYT2 takes up glycine from the extracellular space by an
electrogenic process where this neurotransmitter is co-transported with sodium and chloride …