Affinage

MGAT1

Alpha-1,3-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase · UniProt P26572

Length
445 aa
Mass
50.9 kDa
Annotated
2026-04-28
100 papers in source corpus 16 papers cited in narrative 16 extracted findings

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

MGAT1 encodes two functionally distinct enzymes depending on context: UDP-GlcNAc:α-3-D-mannoside β-1,2-N-acetylglucosaminyltransferase I (GlcNAc-TI), a medial-Golgi glycosyltransferase that catalyzes the first committed step in converting high-mannose N-glycans to complex/hybrid N-glycans (PMID:12634323, PMID:11467936), and an acyl-CoA:monoacylglycerol acyltransferase (MGAT) that synthesizes diacylglycerol from monoacylglycerol and acyl-CoA to promote triacylglycerol biosynthesis (PMID:12077311). In its lipid-metabolic role, MGAT1 localizes to the ER and lipid droplets, interacts physically with DGAT2 to synergistically expand TAG synthesis, and is transcriptionally regulated by PPARγ2 in liver, where its knockdown ameliorates hepatic steatosis (PMID:22869740, PMID:28347400). In its glycosyltransferase role, MGAT1 is essential for embryonic development, oocyte competence, spermatogenesis via ERK1/2 signaling, immune cell encapsulation responses, and suppression of tumor cell invasion; it is specifically inhibited in the Golgi by GnT1IP-L through a luminal-domain heteromeric interaction and can be transcriptionally induced by XBP1s downstream of lactate signaling to drive mitochondrial N-glycosylation in regulatory T cells (PMID:8563140, PMID:15509794, PMID:29386567, PMID:26371870, PMID:39264847, PMID:22829770).

Mechanistic history

Synthesis pass · year-by-year structured walk · 12 steps
  1. 1995 Medium

    Establishing when MGAT1-dependent complex N-glycans first become essential in development: Mgat1-null embryos lose complex N-glycans by E7.5 (maternal glycoproteins sustain them until ~E5.5), linking embryonic lethality to the temporal onset of zygotic MGAT1 expression.

    Evidence In situ hybridization and lectin histochemistry on staged Mgat1-null mouse embryos

    PMID:8563140

    Open questions at the time
    • Specific glycoprotein substrates whose complex N-glycans are required for post-implantation survival are not identified
    • Mechanism of maternal mRNA clearance not characterized
  2. 1997 Medium

    Confirmation that maternally derived wild-type Mgat1 mRNA persists until implantation (~E5.5) and accounts for complex N-glycans in null blastocysts, resolving the apparent paradox of normal early glycosylation in knockouts.

    Evidence RT-PCR on individual PCR-genotyped blastocysts with L-PHA lectin binding

    PMID:9020882 PMID:9363433

    Open questions at the time
    • Translational efficiency of maternal versus zygotic mRNA not compared
    • Gene regulatory elements beyond the proximal promoter remain uncharacterized
  3. 2001 High

    Defining the catalytic mechanism of MGAT1's glycosyltransferase activity: the conserved DXD motif (D212) and R303 are critical for substrate binding, with mutations at these sites causing the Lec1A phenotype, rationalizable by the GlcNAc-TI crystal structure.

    Evidence Site-directed mutagenesis with kinetic analysis of UDP-GlcNAc and Man5GlcNAc2 binding, interpreted against rabbit GlcNAc-TI crystal structure

    PMID:11467936

    Open questions at the time
    • Human MGAT1 crystal structure not yet solved
    • Conformational dynamics upon substrate binding not examined
  4. 2002 High

    MGAT1 was identified as encoding a second, unrelated enzymatic activity — acyl-CoA:monoacylglycerol acyltransferase — that synthesizes diacylglycerol, simultaneously establishing it as a key node in intestinal/hepatic lipid metabolism.

    Evidence Heterologous expression in insect cells with enzymatic activity assay using oleoyl-CoA and monooleoylglycerol substrates

    PMID:12077311

    Open questions at the time
    • Relationship between the glycosyltransferase (GnT-I) MGAT1 gene and the MGAT lipid enzyme MGAT1 gene — these are distinct genes that share the symbol in some nomenclatures; clarity on gene identity needed
    • In vivo substrate specificity for different acyl-CoA and MAG species not fully profiled
  5. 2002 High

    Definitive genetic proof that MGAT1 encodes GlcNAc-TI: reversion mutagenesis of Lec1 CHO cell mutations restored both enzymatic activity and lectin binding, confirming the causal gene-function relationship.

    Evidence Sequencing of Lec1 CHO genomic DNA, reversion by site-directed mutagenesis, enzymatic and lectin-binding assays

    PMID:12634323

    Open questions at the time
    • Whether additional compensatory glycosyltransferases exist in Lec1 cells not explored
  6. 2004 High

    Oocyte-specific deletion revealed that MGAT1 complex N-glycans contribute to zona pellucida thickness and full developmental competence of the egg, but are not strictly required for fertilization.

    Evidence Conditional knockout (ZP3-Cre × Mgat1-flox), lectin staining, and embryo phenotyping

    PMID:15509794

    Open questions at the time
    • Specific zona pellucida glycoprotein targets of MGAT1 not identified
    • Whether the ~25% embryonic defect reflects stochastic or deterministic mechanism unknown
  7. 2010 Medium

    Neuronal MGAT1 activity is a key determinant of organismal lifespan and locomotion in Drosophila, with overexpression extending lifespan up to 135% and conferring oxidative stress resistance — linking complex N-glycan biosynthesis to aging.

    Evidence CNS-specific transgenic rescue/RNAi in Drosophila with GnT1 enzyme activity measurement, oxidative stress and lifespan assays

    PMID:20457894

    Open questions at the time
    • Mammalian relevance of neuronal MGAT1 lifespan extension not tested
    • Neuronal glycoprotein substrates mediating the effect not identified
  8. 2012 Medium

    Multiple advances established MGAT1's roles in hepatic lipid metabolism and cancer: PPARγ2 directly transactivates the MGAT1 promoter to drive hepatic steatosis, MGAT1 knockdown suppresses tumor invasion and metastasis, and Drosophila Mgat1 is required for immune encapsulation.

    Evidence ChIP/EMSA/luciferase for PPARγ2 regulation with in vivo shRNA in mice; shRNA in HeLa/PC-3 cells with orthotopic xenograft; Drosophila loss-of-function immune challenge

    PMID:22829770 PMID:22869740 PMID:22957033

    Open questions at the time
    • Specific surface glycoproteins mediating invasion suppression not identified
    • Whether anti-metastatic effect is cell-type general or restricted to certain cancers unclear
    • Mammalian immune cell phenotype of MGAT1 loss not tested in parallel
  9. 2015 High

    A specific Golgi-resident inhibitor (GnT1IP-L) was shown to selectively inhibit MGAT1 through luminal-domain heteromerization, revealing a dedicated regulatory mechanism for controlling the high-mannose-to-complex N-glycan switch.

    Evidence FRET, BiFC, ER-retention constructs, and enzymatic activity assays in transfected cells

    PMID:26371870

    Open questions at the time
    • Physiological contexts in which GnT1IP-L is upregulated to modulate MGAT1 remain undefined
    • Structural basis of the heteromeric interaction not resolved
  10. 2017 Medium

    MGAT1's lipid-metabolic function was mechanistically elaborated: the enzyme localizes to ER basally and redistributes to lipid droplets under fatty acid loading; its catalytic HPHG motif and N-terminal transmembrane domain are essential; and physical interaction with DGAT2 synergistically enhances TAG synthesis.

    Evidence Immunofluorescence, subcellular fractionation, site-directed mutagenesis, co-immunoprecipitation with DGAT2

    PMID:28347400

    Open questions at the time
    • Reciprocal co-IP for DGAT2 interaction not shown
    • Whether MGAT1-DGAT2 interaction is direct or bridged by other factors unknown
  11. 2018 Medium

    Conditional deletion in spermatogonia revealed that MGAT1-dependent complex N-glycans on basigin activate ERK1/2 signaling to properly time spermiogenesis gene expression, establishing a glycan-to-kinase signaling axis in male fertility.

    Evidence Conditional knockout in mouse spermatogonia, transcriptomics, ERK1/2 phosphorylation comparison in CHO vs Lec1 cells

    PMID:29386567

    Open questions at the time
    • Whether basigin is the sole relevant MGAT1 substrate in germ cells is not established
    • Downstream ERK targets mediating spermiogenesis timing not mapped
  12. 2024 Medium

    An unexpected mitochondrial role for MGAT1 was uncovered: lactate-activated XBP1s upregulates MGAT1, and lactate also facilitates MGAT1 import into mitochondria via TOM70, where it glycosylates progranulin and HYOU1 to enhance Treg oxidative phosphorylation.

    Evidence Mitochondrial isolation, XBP1s ChIP/reporter assay, TOM70 interaction assay, MGAT1 KD, Treg OXPHOS measurement, xenogeneic GvHD mouse model

    PMID:39264847

    Open questions at the time
    • Mitochondrial localization of MGAT1 has not been independently replicated
    • How a Golgi glycosyltransferase accesses mitochondrial substrates mechanistically is not fully resolved
    • Whether mitochondrial N-glycosylation by MGAT1 occurs in cell types beyond Tregs is unknown

Open questions

Synthesis pass · forward-looking unresolved questions
  • Open question: the structural basis of MGAT1 regulation by GnT1IP-L, the full repertoire of physiological glycoprotein substrates in different tissues, and the scope and mechanism of the reported mitochondrial localization remain to be defined.
  • No crystal structure of human MGAT1 in complex with GnT1IP-L
  • Comprehensive substrate identification across tissues lacking
  • Independent confirmation of mitochondrial localization needed

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0016740 transferase activity 4 GO:0140096 catalytic activity, acting on a protein 2
Localization
GO:0005794 Golgi apparatus 2 GO:0005739 mitochondrion 1 GO:0005783 endoplasmic reticulum 1 GO:0005811 lipid droplet 1
Pathway
R-HSA-392499 Metabolism of proteins 4 R-HSA-1266738 Developmental Biology 3 R-HSA-1430728 Metabolism 3 R-HSA-1474165 Reproduction 2 R-HSA-168256 Immune System 2
Partners
BSGDGAT2GNT1IP-LTOM70

Evidence

Reading pass · 16 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2002 MGAT1 encodes an acyl-CoA:monoacylglycerol acyltransferase (MGAT) that catalyzes synthesis of diacylglycerol from monoacylglycerol and acyl-CoA; expression in insect cells markedly increased MGAT activity in cell membranes, and activity was proportional to MGAT1 protein level and substrate concentration. Heterologous expression in insect cells, enzymatic activity assay with substrates oleoyl-CoA and monooleoylglycerol Proceedings of the National Academy of Sciences of the United States of America High 12077311
2012 PPARγ2 directly regulates the MGAT1 promoter to drive hepatic MGAT1 expression; MGAT1 overexpression enhances triglyceride synthesis in hepatocytes, and MGAT1 knockdown in vivo significantly reduces hepatic steatosis in high-fat-fed and ob/ob mice. Luciferase promoter assay, EMSA, ChIP, adenoviral overexpression, shRNA knockdown in mice Proceedings of the National Academy of Sciences of the United States of America High 22869740
2017 MGAT1 localizes to the ER under basal conditions and co-localizes to lipid droplets under fatty acid-enriched conditions; both the N-terminal transmembrane domain and the catalytic HPHG motif are required for enzyme activity; MGAT1 interacts with DGAT2 to synergistically increase TAG biosynthesis and lipid droplet expansion. Subcellular fractionation/immunofluorescence, site-directed mutagenesis of catalytic motif, co-immunoprecipitation with DGAT2 BMB reports Medium 28347400
2002 Lec1 CHO cells lacking GlcNAc-TI (encoded by Mgat1) harbor distinct coding-region mutations causing truncated MGAT1 protein; reversion of mutations by site-directed mutagenesis restores GlcNAc-TI activity and lectin binding, confirming MGAT1 encodes GlcNAc-TI. Sequencing of genomic DNA, site-directed mutagenesis reversion, enzymatic activity assay, lectin binding Glycobiology High 12634323
2001 Two point mutations in the Mgat1-encoded GlcNAc-TI (D212N disrupting the conserved DXD motif; R303W altering a structural element) reduce affinity for both UDP-GlcNAc and Man5GlcNAc2 substrates, causing the Lec1A phenotype; correction by site-directed mutagenesis restores activity, and the effects are rationalized by the crystal structure of rabbit GlcNAc-TI. Site-directed mutagenesis, enzymatic kinetic assay, crystal structure interpretation Biochemistry High 11467936
1997 The human MGAT1 gene is organized with at least two exons; multiple transcription start sites are present in a TATA-less, GC-rich promoter region; CAT reporter assays demonstrate the 5' flanking region of exon 1 drives transcription, consistent with housekeeping gene regulation. Genomic cloning, Northern blot, RNase protection, primer extension, RACE, transient transfection CAT assay The Biochemical journal Medium 9020882
1995 Mgat1-null embryos lack complex N-glycans by E7.5 but retain them at E3.5 due to maternally derived glycoproteins; Mgat1 transcripts increase dramatically between E7.0 and E9.5 preceding embryonic lethality, establishing a temporal requirement for embryonically produced complex N-glycans after implantation. In situ RNA hybridization, lectin histochemistry on staged embryos Glycobiology Medium 8563140
1997 Complex N-glycans in Mgat1-null blastocysts arise from maternally inherited wild-type Mgat1 mRNA that persists until around implantation (E5.5), after which the null phenotype becomes operative; identified by RT-PCR of individual PCR-genotyped blastocysts. PCR genotyping of individual blastocysts, RT-PCR, lectin binding (L-PHA) Glycobiology Medium 9363433
2004 Oocyte-specific deletion of Mgat1 (via ZP3-Cre) produces a thinner zona pellucida lacking complex N-glycans; mutant eggs can be fertilized and implant, but ~25% of resulting embryos are severely retarded, demonstrating that MGAT1-dependent complex N-glycans in oocytes are required for full developmental competence of the egg but not strictly for fertilization or blastogenesis. Conditional knockout (ZP3-Cre × Mgat1-flox), lectin staining, embryo phenotyping Molecular and cellular biology High 15509794
2012 MGAT1 shRNA knockdown in HeLa and PC-3 tumor cells reduces branched N-glycan levels, inhibits cell migration and invasion (without affecting proliferation), alters focal adhesion and microfilament organization, and decreases primary tumor growth and lung metastasis in an orthotopic xenograft model. shRNA knockdown, invasion/migration assay, focal adhesion imaging, orthotopic mouse xenograft PloS one Medium 22957033
2018 Conditional deletion of Mgat1 in spermatogonia causes germ-cell-autonomous infertility; loss of complex N-glycans leads to premature upregulation of spermiogenesis genes and reduced ERK1/2 signaling; basigin (a germ-cell target of MGAT1) activates ERK1/2 in CHO cells but not in Lec1 CHO cells lacking MGAT1. Conditional knockout, Affymetrix gene expression array, IPA/GSEA bioinformatics, ERK1/2 phosphorylation assay in CHO vs Lec1 cells Scientific reports Medium 29386567
2015 GnT1IP-L inhibits MGAT1 specifically in the Golgi via its luminal domain; ER retention of GnT1IP-L reduces inhibitory activity; dynamic FRET and BiFC assays show GnT1IP-L forms homomers in the ER and heteromers with MGAT1 in the Golgi, but not with MGAT2, MGAT3, MGAT4B, or MGAT5. ER-retention constructs, FRET, BiFC, enzymatic activity assays in transfected cells eLife High 26371870
2013 Zinc-finger nuclease (ZFN)-mediated disruption of Mgat1 in CHO cells prevents synthesis of complex N-glycans beyond Man5GlcNAc2, enabling production of recombinant proteins with homogeneous high-mannose glycoforms without impairing cell growth. ZFN genome editing, lectin binding, mass spectrometry glycan profiling Journal of biotechnology Medium 23777858
2024 Elevated intracellular lactate activates XBP1s to upregulate MGAT1 transcription; lactate also interacts with the TOM70 mitochondrial import receptor to facilitate MGAT1 translocation into mitochondria, where MGAT1 drives N-glycosylation of progranulin (GRN) and HYOU1 to enhance Treg oxidative phosphorylation. Mitochondrial isolation, sequencing, XBP1s ChIP/reporter assay, TOM70 interaction assay, MGAT1 KD, Treg OXPHOS measurement, xenogeneic GvHD mouse model The Journal of clinical investigation Medium 39264847
2012 Mgat1-dependent N-glycosylation of Drosophila immune cell membrane proteins is required for the cellular encapsulation response against parasitoid wasps; loss-of-function mutations in Mgat1 (among 8 N-glycosylation pathway genes) lead to defective, disintegrating capsules and reduced parasite resistance. Drosophila genetics (loss-of-function mutants), immune challenge assay, capsule morphology analysis, overexpression rescue PLoS pathogens Medium 22829770
2010 Neuronal expression of Drosophila Mgat1 in the CNS is required for normal locomotion and lifespan; knockdown in CNS neurons recapitulates Mgat1-null locomotor and lifespan defects; neuronal Mgat1 overexpression dramatically extends lifespan (up to 135%) correlating with increased GnT1 activity and oxidative stress resistance. Tissue-specific transgenic rescue and RNAi knockdown in Drosophila, GnT1 enzyme activity assay, oxidative stress assay, lifespan analysis Proceedings of the National Academy of Sciences of the United States of America Medium 20457894

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2005 Localization of the GLYT1 glycine transporter at glutamatergic synapses in the rat brain. Cerebral cortex (New York, N.Y. : 1991) 254 15749988
1995 Regional distribution and developmental variation of the glycine transporters GLYT1 and GLYT2 in the rat CNS. The European journal of neuroscience 243 7582108
2008 Beyond triglyceride synthesis: the dynamic functional roles of MGAT and DGAT enzymes in energy metabolism. American journal of physiology. Endocrinology and metabolism 176 19116371
2002 Identification of a gene encoding MGAT1, a monoacylglycerol acyltransferase. Proceedings of the National Academy of Sciences of the United States of America 162 12077311
2012 Nuclear receptor PPARγ-regulated monoacylglycerol O-acyltransferase 1 (MGAT1) expression is responsible for the lipid accumulation in diet-induced hepatic steatosis. Proceedings of the National Academy of Sciences of the United States of America 142 22869740
1995 Gene structure and glial expression of the glycine transporter GlyT1 in embryonic and adult rodents. The Journal of neuroscience : the official journal of the Society for Neuroscience 125 7891186
1996 Developmental expression of the glycine transporters GLYT1 and GLYT2 in mouse brain. Journal of neurochemistry 102 8667011
2012 6'-Guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment. The Journal of biological chemistry 94 22736766
1995 The role of N-glycosylation in the targeting and activity of the GLYT1 glycine transporter. The Journal of biological chemistry 94 7721869
2002 Five Lec1 CHO cell mutants have distinct Mgat1 gene mutations that encode truncated N-acetylglucosaminyltransferase I. Glycobiology 90 12634323
2003 The glycine neurotransmitter transporter GLYT1 is an organic osmolyte transporter regulating cell volume in cleavage-stage embryos. Proceedings of the National Academy of Sciences of the United States of America 86 14615585
2004 Inactivation of the Mgat1 gene in oocytes impairs oogenesis, but embryos lacking complex and hybrid N-glycans develop and implant. Molecular and cellular biology 84 15509794
2012 Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity. BMC pharmacology 77 22642416
2013 Functional selectivity of 6'-guanidinonaltrindole (6'-GNTI) at κ-opioid receptors in striatal neurons. The Journal of biological chemistry 74 23775075
2008 Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology 74 18602930
2000 Characterization of the interactions between the glycine transporters GLYT1 and GLYT2 and the SNARE protein syntaxin 1A. FEBS letters 70 10722844
1996 Cloning and molecular genetic characterization of the Escherichia coli gntR, gntK, and gntU genes of GntI, the main system for gluconate metabolism. Journal of bacteriology 70 8655507
2006 MS-binding assays: kinetic, saturation, and competitive experiments based on quantitation of bound marker as exemplified by the GABA transporter mGAT1. ChemMedChem 67 16892353
2023 Development of the novel GlyT1 inhibitor, iclepertin (BI 425809), for the treatment of cognitive impairment associated with schizophrenia. European archives of psychiatry and clinical neuroscience 63 36971864
2014 Intestine-specific deletion of acyl-CoA:monoacylglycerol acyltransferase (MGAT) 2 protects mice from diet-induced obesity and glucose intolerance. The Journal of biological chemistry 63 24784138
1999 Molecular cloning and characterization of cDNA coding for beta1, 2N-acetylglucosaminyltransferase I (GlcNAc-TI) from Nicotiana tabacum. Glycobiology 62 10406843
2000 GABA receptor rho1 subunit interacts with a novel splice variant of the glycine transporter, GLYT-1. The Journal of biological chemistry 59 10625616
1997 Analysis of the transmembrane topology of the glycine transporter GLYT1. The Journal of biological chemistry 58 8995423
2012 A novel glycine transporter-1 (GlyT1) inhibitor, ASP2535 (4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole), improves cognition in animal models of cognitive impairment in schizophrenia and Alzheimer's disease. European journal of pharmacology 57 22542656
2011 Pre-synaptic glycine GlyT1 transporter--NMDA receptor interaction: relevance to NMDA autoreceptor activation in the presence of Mg2+ ions. Journal of neurochemistry 57 21348870
2008 Rescue of hippocampal LTP and learning deficits in a rat model of psychosis by inhibition of glycine transporter-1 (GlyT1). The European journal of neuroscience 57 18973561
2003 Pharmacology and expression analysis of glycine transporter GlyT1 with [3H]-(N-[3-(4'-fluorophenyl)-3-(4'phenylphenoxy)propyl])sarcosine. Neuropharmacology 57 12941372
1995 Regulation by phorbol esters of the glycine transporter (GLYT1) in glioblastoma cells. Biochimica et biophysica acta 54 7833348
2006 Molecular identification and characterisation of the glycine transporter (GLYT1) and the glutamine/glutamate transporter (ASCT2) in the rat lens. Experimental eye research 51 16635486
2000 Isolation and characterization of plant N-acetyl glucosaminyltransferase I (GntI) cDNA sequences. Functional analyses in the Arabidopsis cgl mutant and in antisense plants. Plant physiology 50 10889259
2010 Glycine transporter GLYT1 is essential for glycine-mediated protection of human intestinal epithelial cells against oxidative damage. The Journal of physiology 48 20123783
2008 Inhibitors of GlyT1 affect glycine transport via discrete binding sites. Molecular pharmacology 48 18815213
2007 Functional expression of release-regulating glycine transporters GLYT1 on GABAergic neurons and GLYT2 on astrocytes in mouse spinal cord. Neurochemistry international 48 17597258
2010 Functional 'glial' GLYT1 glycine transporters expressed in neurons. Journal of neurochemistry 47 20477934
2005 The scaffolding protein PSD-95 interacts with the glycine transporter GLYT1 and impairs its internalization. Journal of neurochemistry 44 16271045
2002 Kappa opioid antagonist effects of the novel kappa antagonist 5'-guanidinonaltrindole (GNTI) in an assay of schedule-controlled behavior in rhesus monkeys. Psychopharmacology 44 12373442
1994 Carboxyl terminus of the glycine transporter GLYT1 is necessary for correct processing of the protein. The Journal of biological chemistry 43 7961780
2024 Lactate supports Treg function and immune balance via MGAT1 effects on N-glycosylation in the mitochondria. The Journal of clinical investigation 41 39264847
2015 BDNF, via truncated TrkB receptor, modulates GlyT1 and GlyT2 in astrocytes. Glia 41 26200505
2012 Mgat1-dependent N-glycosylation of membrane components primes Drosophila melanogaster blood cells for the cellular encapsulation response. PLoS pathogens 41 22829770
2004 Bergmann glial GlyT1 mediates glycine uptake and release in mouse cerebellar slices. The Journal of physiology 41 15331688
2013 Engineering Chinese hamster ovary (CHO) cells for producing recombinant proteins with simple glycoforms by zinc-finger nuclease (ZFN)-mediated gene knockout of mannosyl (alpha-1,3-)-glycoprotein beta-1,2-N-acetylglucosaminyltransferase (Mgat1). Journal of biotechnology 40 23777858
2009 Linkage and genome-wide association analysis of obesity-related phenotypes: association of weight with the MGAT1 gene. Obesity (Silver Spring, Md.) 39 19851299
2008 Design of potent GlyT1 inhibitors: in vitro and in vivo profiles. Current opinion in molecular therapeutics 39 19051137
1997 Molecular genetic characterization of the Escherichia coli gntT gene of GntI, the main system for gluconate metabolism. Journal of bacteriology 38 9045817
2006 Progress in the preparation and testing of glycine transporter type-1 (GlyT1) inhibitors. Current topics in medicinal chemistry 37 17017963
2004 Blockade of glycine transporter-1 (GLYT-1) potentiates NMDA receptor-mediated synaptic transmission in hypoglossal motorneurons. Journal of neurophysiology 37 15175365
2019 Bitopertin, a selective oral GLYT1 inhibitor, improves anemia in a mouse model of β-thalassemia. JCI insight 35 31593554
1995 Complex asparagine-linked oligosaccharides in Mgat1-null embryos. Glycobiology 35 8563140
2018 CRISPR/Cas9 gene editing for the creation of an MGAT1-deficient CHO cell line to control HIV-1 vaccine glycosylation. PLoS biology 34 30157178
2024 GNTI-122: an autologous antigen-specific engineered Treg cell therapy for type 1 diabetes. JCI insight 33 38516892
2022 QSAR, ADMET In Silico Pharmacokinetics, Molecular Docking and Molecular Dynamics Studies of Novel Bicyclo (Aryl Methyl) Benzamides as Potent GlyT1 Inhibitors for the Treatment of Schizophrenia. Pharmaceuticals (Basel, Switzerland) 33 35745588
2010 Glycine transporter (GlyT1) inhibitors with reduced residence time increase prepulse inhibition without inducing hyperlocomotion in DBA/2 mice. Biochemical pharmacology 33 20637735
2008 Mechanisms of endoplasmic-reticulum export of glycine transporter-1 (GLYT1). The Biochemical journal 33 17919119
2015 GlyT-1 Inhibition Attenuates Attentional But Not Learning or Motivational Deficits of the Sp4 Hypomorphic Mouse Model Relevant to Psychiatric Disorders. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology 32 25907107
2012 Suppression of cancer progression by MGAT1 shRNA knockdown. PloS one 32 22957033
2000 Expression of glycine and the glycine transporter glyt-1 in the developing rat retina. Visual neuroscience 32 10750822
2018 Expression of functional inhibitory neurotransmitter transporters GlyT1, GAT-1, and GAT-3 by astrocytes of inferior colliculus and hippocampus. Molecular brain 31 29370841
2013 GlyT1 and GlyT2 in brain astrocytes: expression, distribution and function. Brain structure & function 31 23529192
2010 Recent progress in the discovery of non-sarcosine based GlyT1 inhibitors. Current topics in medicinal chemistry 31 20166956
2010 Blockade of glycine transporter (GlyT) 2, but not GlyT1, ameliorates dynamic and static mechanical allodynia in mice with herpetic or postherpetic pain. Journal of pharmacological sciences 31 20173309
1997 Complex N-glycans in Mgat1 null preimplantation embryos arise from maternal Mgat1 RNA. Glycobiology 31 9363433
2018 Multiple Rising Doses of Oral BI 425809, a GlyT1 Inhibitor, in Young and Elderly Healthy Volunteers: A Randomised, Double-Blind, Phase I Study Investigating Safety and Pharmacokinetics. Clinical drug investigation 30 29846887
2013 Hypomorphic MGAT5 polymorphisms promote multiple sclerosis cooperatively with MGAT1 and interleukin-2 and 7 receptor variants. Journal of neuroimmunology 29 23351704
2010 Mgat1-dependent N-glycans are essential for the normal development of both vertebrate and invertebrate metazoans. Seminars in cell & developmental biology 29 20206280
1997 Organization of the human beta-1,2-N-acetylglucosaminyltransferase I gene (MGAT1), which controls complex and hybrid N-glycan synthesis. The Biochemical journal 29 9020882
1997 Neuronal dependency of the glycine transporter GLYT1 expression in glial cells. Glia 28 9179600
2015 Supplementation of antipsychotic treatment with sarcosine – GlyT1 inhibitor – causes changes of glutamatergic (1)NMR spectroscopy parameters in the left hippocampus in patients with stable schizophrenia. Neuroscience letters 27 26306650
2013 Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Current pharmaceutical design 27 23194655
2010 Neuronal expression of Mgat1 rescues the shortened life span of Drosophila Mgat11 null mutants and increases life span. Proceedings of the National Academy of Sciences of the United States of America 27 20457894
2006 Inhibition of the glycine transporter GlyT-1 potentiates the effect of risperidone, but not clozapine, on glutamatergic transmission in the rat medial prefrontal cortex. Synapse (New York, N.Y.) 27 16715496
2023 Functional crosstalk of the glycine transporter GlyT1 and NMDA receptors. Neuropharmacology 26 37003571
2021 Chloride-dependent conformational changes in the GlyT1 glycine transporter. Proceedings of the National Academy of Sciences of the United States of America 26 33658361
2016 The G-protein biased partial κ opioid receptor agonist 6'-GNTI blocks hippocampal paroxysmal discharges without inducing aversion. British journal of pharmacology 26 26928671
2016 Effects of GlyT1 inhibition on erythropoiesis and iron homeostasis in rats. Experimental hematology 25 27403535
2009 Comparative genomics and proteomics of vertebrate diacylglycerol acyltransferase (DGAT), acyl CoA wax alcohol acyltransferase (AWAT) and monoacylglycerol acyltransferase (MGAT). Comparative biochemistry and physiology. Part D, Genomics & proteomics 25 20374941
2004 The synthesis and SAR of 2-arylsulfanyl-phenyl piperazinyl acetic acids as glyT-1 inhibitors. Bioorganic & medicinal chemistry letters 25 15225720
2011 Characterization of [11C]RO5013853, a novel PET tracer for the glycine transporter type 1 (GlyT1) in humans. NeuroImage 24 22155032
2013 Selective κ opioid antagonists nor-BNI, GNTI and JDTic have low affinities for non-opioid receptors and transporters. PloS one 23 23976952
2003 The activator of GntII genes for gluconate metabolism, GntH, exerts negative control of GntR-regulated GntI genes in Escherichia coli. Journal of bacteriology 23 12618441
2000 Differential effects of ethanol on glycine uptake mediated by the recombinant GLYT1 and GLYT2 glycine transporters. British journal of pharmacology 23 10683205
2014 Functional analysis of the inhibitory neurotransmitter transporters GlyT1, GAT-1, and GAT-3 in astrocytes of the lateral superior olive. Glia 21 25103283
2001 Independent Lec1A CHO glycosylation mutants arise from point mutations in N-acetylglucosaminyltransferase I that reduce affinity for both substrates. Molecular consequences based on the crystal structure of GlcNAc-TI. Biochemistry 21 11467936
2015 GnT1IP-L specifically inhibits MGAT1 in the Golgi via its luminal domain. eLife 20 26371870
2012 The chromatin-binding protein HMGN3 stimulates histone acetylation and transcription across the Glyt1 gene. The Biochemical journal 20 22150271
2008 The glycine transporter 1 gene (GLYT1) is associated with methamphetamine-use disorder. American journal of medical genetics. Part B, Neuropsychiatric genetics : the official publication of the International Society of Psychiatric Genetics 20 17582620
2001 Glycine supply to human enterocytes mediated by high-affinity basolateral GLYT1. Gastroenterology 20 11159884
2019 The Golgi Localization of GnTI Requires a Polar Amino Acid Residue within Its Transmembrane Domain. Plant physiology 19 30971450
2015 Expression and purification of soluble and stable ectodomain of natural killer cell receptor LLT1 through high-density transfection of suspension adapted HEK293S GnTI(-) cells. Protein expression and purification 19 25623399
2012 Interactions between glycine transporter type 1 (GlyT-1) and some inhibitor molecules - glycine transporter type 1 and its inhibitors (review). Acta physiologica Hungarica 19 22425803
2009 Interactions between the glycine transporter 1(GlyT1) inhibitor SSR504734 and psychoactive drugs in mouse motor behaviour. European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology 19 19282154
2009 The glycine transporter GlyT1 controls N-methyl-D-aspartic acid receptor coagonist occupancy in the mouse retina. The European journal of neuroscience 19 20092573
2005 The glycine transporter GLYT1 interacts with Sec3, a component of the exocyst complex. Neuropharmacology 19 16181645
2023 Transmembrane Protein 68 Functions as an MGAT and DGAT Enzyme for Triacylglycerol Biosynthesis. International journal of molecular sciences 18 36768334
2022 Synergistic Control of Transmitter Turnover at Glycinergic Synapses by GlyT1, GlyT2, and ASC-1. International journal of molecular sciences 18 35269698
2018 MGAT1 and Complex N-Glycans Regulate ERK Signaling During Spermatogenesis. Scientific reports 18 29386567
2017 Monoacylglycerol O-acyltransferase 1 (MGAT1) localizes to the ER and lipid droplets promoting triacylglycerol synthesis. BMB reports 18 28347400
2016 Molecular switches of the κ opioid receptor triggered by 6'-GNTI and 5'-GNTI. Scientific reports 18 26742690
2006 The synthesis and SAR of 2-arylsulfanylphenyl-1-oxyalkylamino acids as GlyT-1 inhibitors. Bioorganic & medicinal chemistry letters 18 16725323
2006 Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability. Bioorganic & medicinal chemistry letters 18 16757170