Sodium- and chloride-dependent glycine transporter 1, also known as glycine transporter 1, is a
protein
Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residue (biochemistry), residues. Proteins perform a vast array of functions within organisms, including Enzyme catalysis, catalysing metab ...
that in humans is encoded by the ''SLC6A9''
gene
In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
which is promising therapeutic target for treatment of diabetes and obesity.
Selective inhibitors
Elevation of extracellular synaptic
glycine
Glycine (symbol Gly or G; ) is an amino acid that has a single hydrogen atom as its side chain. It is the simplest stable amino acid. Glycine is one of the proteinogenic amino acids. It is encoded by all the codons starting with GG (G ...
concentration by blockade of GlyT1 has been hypothesized to potentiate
NMDA receptor
The ''N''-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and predominantly Ca2+ ion channel found in neurons. The NMDA receptor is one of three types of ionotropic glutamate receptors, the other ...
function in vivo and to represent a rational approach for the treatment of
schizophrenia
Schizophrenia () is a mental disorder characterized variously by hallucinations (typically, Auditory hallucination#Schizophrenia, hearing voices), delusions, thought disorder, disorganized thinking and behavior, and Reduced affect display, f ...
and cognitive disorders. Several drug candidates have reached clinical trials.
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ASP2535
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Bitopertin (RG1678), which has entered
phase II trials for the treatment of schizophrenia
* Iclepertin (
BI 425809
Iclepertin (developmental code name BI 425809) is an investigational nootropic to enhance the cognition and functional capacity in schizophrenia developed by Boehringer Ingelheim. As of May 2020, it is in phase III of clinical trial under the co ...
) by Boehringer Ingelheim which is thought to improve cognitive impairment due to schizophrenia
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Org 25935 (Sch 900435)
* PF-03463275 (in phase II trial)
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Pesampator (PF-04958242) by Pfizer
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Sarcosine
Sarcosine, also known as ''N''-methylglycine, or monomethylglycine, is a amino acid with the formula CH3N(H)CH2CO2H. It exists at neutral pH as the zwitterion CH3N+(H)2CH2CO2−, which can be obtained as a white, water-soluble powder. Like some ...
which is thought to improve cognitive impairment due to schizophrenia
Pathological mutations
Mutations of the gene may cause a severe metabolic disorder discovered in 2016 and called
glycine encephalopathy with normal serum glycine (
OMIM
Online Mendelian Inheritance in Man (OMIM) is a continuously updated catalog of human genes and genetic disorders and traits, with a particular focus on the gene-phenotype relationship. , approximately 9,000 of the over 25,000 entries in OMIM ...
617301), also known as GlyT1 encephalopathy.
See also
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Sodium:neurotransmitter symporter
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Solute carrier family
The solute carrier (SLC) group of membrane transport proteins include over 400 members organized into 66 families. Most members of the SLC group are located in the cell membrane. The SLC gene nomenclature system was originally proposed by the HUGO ...
References
Further reading
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Solute carrier family
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