Affinage

PNPO

Pyridoxine-5'-phosphate oxidase · UniProt Q9NVS9

Length
261 aa
Mass
30.0 kDa
Annotated
2026-06-10
26 papers in source corpus 16 papers cited in narrative 15 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 5/5 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

PNPO encodes pyridox(am)ine 5'-phosphate oxidase, the rate-limiting FMN-dependent enzyme that oxidizes pyridoxine 5'-phosphate (PNP) and pyridoxamine 5'-phosphate (PMP) to pyridoxal 5'-phosphate (PLP), the active vitamin B6 cofactor (PMID:9601034, PMID:31759955). Loss-of-function mutations — including null splice-site and stop-codon alleles and activity-reducing missense changes — cause neonatal epileptic encephalopathy, with pathogenicity established by reduced enzymatic activity in cell expression and recombinant systems; many disease residues map to FMN-cofactor or PLP-product binding sites, and partial-function variants act by lowering FMN affinity, destabilizing the protein, and impairing transfer of PLP to downstream apoenzymes (PMID:15772097, PMID:24645144, PMID:28818555, PMID:29379851). In vivo, PNPO loss depletes PLP and pyridoxal while PMP and pyridoxamine accumulate, lowering PLP-dependent synthesis of GABA, glutamate, and glycine; PLP supplementation rescues neurotransmitter levels and behavioral and seizure phenotypes, placing PNPO upstream of inhibitory neurotransmitter metabolism (PMID:31759955, PMID:31616300, PMID:35217610). PNPO functions cell-autonomously in GABAergic neurons to support survival and suppress seizures (PMID:41296493). Beyond canonical B6 metabolism, PNPO activity serves as an oxygen sensor in macrophages, where hypoxic loss of PLP impairs lysosomal acidification and supersulfide synthesis and delays inflammatory resolution (PMID:38822028); PNPO oxidizes Disheveled-3 at Met282 to activate Wnt/β-catenin signaling in myeloma via residues R95 and K117 (PMID:39656865); and it promotes autophagic flux and lysosomal biogenesis through a PNPO–LAMP2 axis in cancer cells (PMID:38615082).

Mechanistic history

Synthesis pass · year-by-year structured walk · 9 steps
  1. 1998 High

    Established that the PNPO cDNA encodes a functional, rate-limiting enzyme of PLP biosynthesis, defining the gene's core catalytic identity.

    Evidence stable transfection of PNPO-negative hepatoma cell lines with enzymatic and immunological readout

    PMID:9601034

    Open questions at the time
    • No structural model of the enzyme
    • Cofactor and oligomeric requirements not defined here
  2. 2005 High

    Linked PNPO loss-of-function to human disease by showing patient mutations abolish or markedly reduce catalytic activity, establishing causality for a vitamin B6-responsive encephalopathy.

    Evidence expression of patient splice, nonsense, and missense alleles in CHO cells with activity assays

    PMID:15772097

    Open questions at the time
    • Mechanism connecting PLP depletion to seizures not yet shown
    • No in vivo model
  3. 2008 Medium

    Extended the genotype-activity map with an additional missense allele retaining residual activity, refining understanding of partial loss-of-function.

    Evidence expression studies and quantitative enzyme assay of p.Arg95His

    PMID:18485777

    Open questions at the time
    • Single mutation
    • No structural rationale provided
  4. 2014 Medium

    Mapped pathogenic residues onto FMN-cofactor and PLP-product binding sites, building a structure-function basis for how mutations impair catalysis.

    Evidence cell-free expression with mass-spectrometry activity assay and CHO-K1 expression across multiple mutations

    PMID:24645144 PMID:24658933

    Open questions at the time
    • No high-resolution structure of mutant enzymes
    • Binding affinities not directly measured
  5. 2017 High

    Defined a precise biochemical mechanism for partial loss of function, showing a variant reduces FMN affinity and thermal stability and impairs PLP delivery to apoenzymes without globally unfolding the protein.

    Evidence recombinant protein kinetics, FMN/PLP binding constants, and thermal stability assays

    PMID:28818555 PMID:29379851

    Open questions at the time
    • Single variant characterized in depth
    • Mechanism of PLP channeling to apoenzymes not resolved
  6. 2019 High

    Demonstrated in vivo that PNPO loss shifts the B6 vitamer balance and depletes GABA and glutamate, with PLP rescue, directly tying enzyme deficiency to neurotransmitter metabolism and brain phenotypes.

    Evidence CRISPR/Cas9 knockout and morpholino knockdown zebrafish with vitamer/neurotransmitter profiling, mRNA and PLP/pyridoxamine rescue; plus Drosophila sgll RNAi with chromosome and glucose phenotypes

    PMID:31506944 PMID:31616300 PMID:31759955

    Open questions at the time
    • Residual phenotypes after PLP rescue point to unexplained PMP-related effects
    • Drosophila DNA-integrity/glucose link not validated in mammals
  7. 2022 High

    Established allele-dependent genotype-phenotype correlation and a dominant-negative mechanism in vivo, showing biochemical severity predicts organismal seizure and survival outcomes.

    Evidence CRISPR knock-in Drosophila carrying human epilepsy variants with behavioral assays and PLP dietary rescue

    PMID:35217610

    Open questions at the time
    • Molecular basis of dominant-negative effect (e.g., dimer poisoning) not directly demonstrated
    • Mammalian confirmation lacking
  8. 2024 Medium

    Revealed non-canonical roles: PNPO activity senses oxygen to control lysosomal acidification and inflammation, directly oxidizes DVL3 to drive Wnt signaling, and supports autophagy via a LAMP2 axis, expanding PNPO beyond a metabolic housekeeping enzyme.

    Evidence macrophage hypoxia model with lysosomal/TET2/iron/supersulfide readouts; celastrol-probe target ID, co-IP, PNPO R95/K117 mutagenesis, DVL3 oxidation and xenografts; siRNA/overexpression with LAMP2 epistasis and cell-cycle analysis

    PMID:38615082 PMID:38822028 PMID:39656865

    Open questions at the time
    • Each non-canonical role characterized in a single context/lab
    • How a B6 oxidase oxidizes a protein methionine substrate mechanistically unresolved
    • Relationship between metabolic and signaling functions unclear
  9. 2025 High

    Localized PNPO's neurological function to GABAergic neurons cell-autonomously and showed a functional interaction with alcohol at the level of inhibitory neurotransmitter metabolism.

    Evidence cell-type-specific hPNPO rescue in Drosophila sgll mutants with GABA-receptor pharmacology; PNPO-deficient flies with alcohol behavioral assays and VB6 rescue (the alcohol study is a preprint)

    PMID:41296493 PMID:bio_10.1101_2025.03.06.641947

    Open questions at the time
    • Partial glial rescue not mechanistically explained
    • Mammalian cell-type-specific requirement not tested
    • Alcohol interaction is preprint-stage

Open questions

Synthesis pass · forward-looking unresolved questions
  • How PNPO's metabolic (PLP-generating) and non-canonical (protein-oxidizing, oxygen-sensing, lysosome-regulating) activities are integrated within a single enzyme remains unresolved.
  • No structure of PNPO bound to non-canonical substrates such as DVL3
  • Unclear whether signaling functions depend on PLP output or are catalytically independent
  • Mammalian validation of expanded roles pending

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0016491 oxidoreductase activity 4 GO:0016740 transferase activity 2
Pathway
R-HSA-1430728 Metabolism 3 R-HSA-112316 Neuronal System 2 R-HSA-162582 Signal Transduction 1
Partners

Evidence

Reading pass · 15 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2005 PNPO encodes pyridox(am)ine 5'-phosphate oxidase, the enzyme responsible for converting pyridoxamine 5'-phosphate and pyridoxine 5'-phosphate to pyridoxal 5'-phosphate (PLP). Splice site (IVS3-1g>a) and stop codon (X262Q) mutations in PNPO were null activity mutations, and the missense mutation R229W markedly reduced enzymatic activity, as demonstrated by expression studies in Chinese hamster ovary cells. Expression studies in CHO cells, enzymatic activity assays, PNPO gene sequencing Human molecular genetics High 15772097
1998 PNPO cDNA encodes a functional pyridoxine-5'-phosphate oxidase; stable transfection of PNPO-negative hepatoma cell lines with the PNPO cDNA restored enzymatically active PNPO protein, confirming the cDNA encodes the rate-limiting enzyme in PLP biosynthesis. The translated product was immunologically reactive to a polyclonal PNPO antibody. Stable transfection of PNPO-negative hepatoma cell lines, enzymatic activity assay, immunological verification Biochemistry High 9601034
2014 Novel PNPO sequence changes, including R225H/C and D33V mutations, were shown to reduce enzyme activity using a cell-free expression system and a mass spectrometry-based assay for pyridoxamine phosphate oxidase. Many mutations affected residues involved in binding FMN (cofactor) or PLP (product), establishing structure-function relationships for these residues. Cell-free expression system, mass spectrometry-based enzymatic assay Brain : a journal of neurology Medium 24645144
2014 The PNPO missense mutations p.Arg225His and p.Arg141Cys, and the deletion c.279_290del, were shown to reduce enzymatic activity by expression studies in CHO-K1 cell lines, establishing their pathogenicity. These mutations were absent in 100 control alleles. Expression studies in CHO-K1 cell lines, enzymatic activity assay Neurology Medium 24658933
2008 The novel PNPO mutation c.284G>A (p.Arg95His) in exon 3 reduces PNPO mutant enzymatic activity to 18% relative to wild type, as demonstrated by expression studies. Expression studies, enzymatic activity assay Molecular genetics and metabolism Medium 18485777
2017 The Arg116Gln PNPO variant, expressed as recombinant protein, does not alter overall enzyme structure but reduces affinity for the cofactor FMN, reduces thermal stability, slightly affects catalytic efficiency, and impairs transfer of PLP to PLP-dependent enzymes, establishing a mechanistic basis for partial loss of function. Recombinant protein expression, structural and kinetic characterization, FMN and PLP binding constants, thermal stability assay Molecular genetics and metabolism High 28818555 29379851
2019 In Drosophila, silencing the PNPO ortholog sgll (sugarlethal) by RNAi causes chromosome aberrations in neuroblasts and induces diabetic hallmarks (hyperglycemia, small body size). Chromosome aberrations are largely caused by the genotoxic effect of advanced glycation end products triggered by high glucose, establishing that PNPO/PLP is required for both DNA integrity and glucose homeostasis. RNAi knockdown in Drosophila, chromosome aberration analysis, glucose measurement Journal of cellular physiology Medium 31506944
2019 CRISPR/Cas9-generated pnpo-/- zebrafish show reduction of PLP and pyridoxal with accumulation of PMP and pyridoxamine, confirming PNPO catalyzes the oxidation of PNP and PMP to PLP in vivo. Decreased GABA and glutamate result from impaired PLP-dependent enzyme activity. PLP treatment normalized PLP, glutamate, GABA, and glycine levels but did not normalize all amino acid profiles, suggesting additional roles for PMP accumulation in the disease phenotype. CRISPR/Cas9 knockout zebrafish, biochemical profiling (B6 vitamers, amino acids, neurotransmitters), PLP rescue Biochimica et biophysica acta. Molecular basis of disease High 31759955
2019 Zebrafish pnpo knockdown (morpholino) causes brain malformation and impaired locomotor activity. These phenotypes are rescued by co-injection of zpnpo or hPNPO mRNA, or by PLP supplementation. Pyridoxamine (PM) supplementation showed rescue effects at lower concentrations than PLP, suggesting PM as an alternative substrate/therapeutic route. GABA supplementation also showed partial rescue, placing PNPO upstream of GABA synthesis. Morpholino knockdown in zebrafish, mRNA rescue, pharmacological supplementation, behavioral assay Frontiers in pharmacology Medium 31616300
2022 CRISPR-Cas9 knock-in Drosophila alleles carrying human PNPO epilepsy-associated variants (h116, h33, h95) exhibit allele-dependent phenotypes (developmental impairments, seizures, shortened lifespan) correlating with the known biochemical severity of each mutation. The hR95H allele has a dominant-negative effect, rendering heterozygous flies susceptible to seizures and premature death. PLP supplementation prevented developmental impairments and seizures. CRISPR-Cas9 knock-in Drosophila, behavioral analysis, PLP dietary supplementation rescue Proceedings of the National Academy of Sciences of the United States of America High 35217610
2024 PNPO acts as an oxygen sensor in macrophages: decreased PNPO activity under prolonged hypoxia reduces PLP levels, inhibiting lysosomal acidification. This leads to iron dysregulation, TET2 protein loss, and delayed resolution of inflammatory response. Among PLP-dependent metabolic pathways, supersulfide synthesis is specifically suppressed under prolonged hypoxia, mechanistically linking PNPO activity to lysosomal function and macrophage inflammatory phenotype. Macrophage hypoxia model, PNPO activity assay, lysosomal acidification assay, iron and TET2 protein measurement, supersulfide metabolite profiling Nature metabolism High 38822028
2024 PNPO oxidizes disheveled 3 at Met282 (DVL3M282), leading to abnormal activation of the Wnt/β-catenin pathway in multiple myeloma cells. Critical PNPO residues R95 and K117 are required for interaction with DVL3. Disrupting the PNPO-DVL3 interaction (with Eltrombopag) inhibited MM cell growth and reduced bone lesions in mouse models. Celastrol probe target identification, co-IP/interaction studies, mutagenesis of PNPO (R95, K117), Wnt/β-catenin pathway reporter, mouse xenograft model, DVL3 oxidation assay Advanced science (Weinheim, Baden-Wurttemberg, Germany) Medium 39656865
2024 PNPO promotes lysosomal biogenesis and perinuclear distribution, enhancing autophagic flux in ovarian cancer cells via a PNPO-LAMP2 axis. LAMP2 silencing blocked PNPO's effect on cellular processes. PNPO also regulates cell cycle progression via cyclin B1 and phosphorylated CDK1. siRNA knockdown, overexpression, LAMP2 co-silencing, cell cycle analysis, xenograft tumor model Apoptosis : an international journal on programmed cell death Medium 38615082
2025 In Drosophila sgll (PNPO ortholog) mutants, cell-autonomous expression of human PNPO cDNA specifically in GABAergic neurons largely restored lifespan and attenuated seizure activity, while expression in cholinergic or glutamatergic neurons did not. Glial expression provided partial rescue. GABA-B agonist SKF-97541 (but not GABA-A modulators) reduced mortality, establishing that PNPO acts cell-autonomously in GABAergic neurons to support brain function. Cell-type-specific hPNPO cDNA rescue in Drosophila sgll mutants, survival and seizure behavioral assays, pharmacological GABA receptor modulation Journal of neurogenetics High 41296493
2025 In Drosophila PNPO (sgll) mutants, PNPO deficiency reduces alcohol aversion, increases alcohol consumption, and alters locomotor behavior. Biochemically, both PNPO deficiency and alcohol exposure elevate GABA and glycine. VB6 supplementation rescues lethality caused by combined PNPO deficiency and alcohol, establishing a functional interaction between genetic VB6 deficiency and alcohol at the level of inhibitory neurotransmitter metabolism. Drosophila PNPO mutant model, behavioral assays (alcohol aversion, consumption, locomotion), amino acid/neurotransmitter metabolomics, VB6 supplementation rescue bioRxivpreprint Medium bio_10.1101_2025.03.06.641947

Source papers

Stage 0 corpus · 26 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2005 Neonatal epileptic encephalopathy caused by mutations in the PNPO gene encoding pyridox(am)ine 5'-phosphate oxidase. Human molecular genetics 219 15772097
2014 Epilepsy due to PNPO mutations: genotype, environment and treatment affect presentation and outcome. Brain : a journal of neurology 144 24645144
2014 Pyridoxine responsiveness in novel mutations of the PNPO gene. Neurology 75 24658933
2007 A new fatal case of pyridox(am)ine 5'-phosphate oxidase (PNPO) deficiency. Molecular genetics and metabolism 48 18024216
2008 PNPO deficiency: an under diagnosed inborn error of pyridoxine metabolism. Molecular genetics and metabolism 43 18485777
2012 Partial Pyridoxine Responsiveness in PNPO Deficiency. JIMD reports 36 23430561
1998 Absence of pyridoxine-5'-phosphate oxidase (PNPO) activity in neoplastic cells: isolation, characterization, and expression of PNPO cDNA. Biochemistry 31 9601034
2017 Pyridoxine-5'-phosphate oxidase (Pnpo) deficiency: Clinical and biochemical alterations associated with the C.347g>A (P.·Arg116gln) mutation. Molecular genetics and metabolism 29 28818555
2016 Pyridoxine responsive epilepsy caused by a novel homozygous PNPO mutation. Molecular genetics and metabolism reports 28 27014579
2019 Pyridoxine/pyridoxamine 5'-phosphate oxidase (Sgll/PNPO) is important for DNA integrity and glucose homeostasis maintenance in Drosophila. Journal of cellular physiology 24 31506944
2019 Pyridox(am)ine 5'-phosphate oxidase (PNPO) deficiency in zebrafish results in fatal seizures and metabolic aberrations. Biochimica et biophysica acta. Molecular basis of disease 22 31759955
2015 PNPO Deficiency and Cirrhosis: Expanding the Clinical Phenotype? JIMD reports 21 26108646
2015 Normal Cerebrospinal Fluid Pyridoxal 5'-Phosphate Level in a PNPO-Deficient Patient with Neonatal-Onset Epileptic Encephalopathy. JIMD reports 18 25762494
2024 PNPO-PLP axis senses prolonged hypoxia in macrophages by regulating lysosomal activity. Nature metabolism 15 38822028
2022 Drosophila carrying epilepsy-associated variants in the vitamin B6 metabolism gene PNPO display allele- and diet-dependent phenotypes. Proceedings of the National Academy of Sciences of the United States of America 15 35217610
2015 Pyridoxal 5ꞌ-phosphate-responsive epilepsy with novel mutations in the PNPO gene: a case report. Genetics and molecular research : GMR 13 26535729
2024 PNPO-Mediated Oxidation of DVL3 Promotes Multiple Myeloma Malignancy and Osteoclastogenesis by Activating the Wnt/β-Catenin Pathway. Advanced science (Weinheim, Baden-Wurttemberg, Germany) 11 39656865
2017 Biochemical data from the characterization of a new pathogenic mutation of human pyridoxine-5'-phosphate oxidase (PNPO). Data in brief 11 29379851
2020 Variable treatment response in a patient with pyridoxal N phosphate oxidase (PNPO) deficiency- understanding the paradox. Epilepsy & behavior reports 8 32395712
2019 Pyridoxamine Supplementation Effectively Reverses the Abnormal Phenotypes of Zebrafish Larvae With PNPO Deficiency. Frontiers in pharmacology 7 31616300
2007 Association between PNPO and schizophrenia in the Japanese population. Schizophrenia research 7 17851041
2024 Targeting PNPO to suppress tumor growth via inhibiting autophagic flux and to reverse paclitaxel resistance in ovarian cancer. Apoptosis : an international journal on programmed cell death 6 38615082
2026 Repurposing Hetrombopag for Multiple Myeloma by Targeting PNPO: A Celastrol-Inspired Approach. Basic & clinical pharmacology & toxicology 0 41914238
2026 Should PNPO Deficiency Be Treated In Utero? Clinical Findings From Prenatal Pyridoxine Therapy. JIMD reports 0 42016347
2026 Integration of Multi-Omics Data Identifies the Role of the Selenium-Related Gene PNPO and Pre-exhausted CD127- CD8+ T Cells in Laryngeal Carcinoma. Cancer informatics 0 42027653
2025 A cell-autonomous role for the vitamin B6 metabolism gene PNPO in Drosophila GABAergic neurons. Journal of neurogenetics 0 41296493

Missed literature

Know a paper Affinage missed for PNPO? Flag it for the maintainers and the community.

No submissions yet.