Affinage

AGMAT

Guanidino acid hydrolase, mitochondrial · UniProt Q9BSE5

Length
352 aa
Mass
37.7 kDa
Annotated
2026-06-09
33 papers in source corpus 11 papers cited in narrative 11 extracted findings
Cross-family judge vs UniProt: tie faithfulness: 4/4 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

AGMAT is a metabolic hydrolase that in humans acts on linear guanidino acids rather than agmatine, hydrolyzing taurocyamine, guanidinobutyrate, guanidinopropionate, and guanidinoacetate while remaining virtually inactive toward agmatine, and operates downstream of the amidinotransferase GATM in guanidino acid catabolism (PMID:36543883). In a parallel developmental context, AGMAT functions in the alternative ADC/AGMAT polyamine-biosynthesis route that converts arginine via agmatine to putrescine; in vivo knockdown in ovine conceptuses impairs polyamine synthesis and produces non-elongated, morphologically abnormal conceptuses with reduced pregnancy rates, establishing its requirement during peri-implantation development (PMID:24648395, PMID:29196820). In the brain, AGMAT is expressed in parvalbumin- and somatostatin-positive hippocampal and cortical interneurons where it degrades agmatine, and its overexpression or loss bidirectionally modulates Schaffer collateral-CA1 excitatory transmission and mood-related behaviors (PMID:36849038, PMID:27404284). In cancer, AGMAT is a c-Myc-driven, miR-151a-5p-targeted oncogenic effector that promotes proliferation and metastasis through iNOS/NO-dependent MAPK and PI3K/AKT signaling and through TGFβ/Smad-driven EMT (PMID:31699997, PMID:35837051, PMID:36680755, PMID:36704851); within the tumor microenvironment, exosomal miR-33a suppresses AGMAT in cancer-associated fibroblasts to lower putrescine and remodel stromal stress-granule biology (PMID:40903826). AGMAT also physically associates with the urea-cycle enzyme CPS1 in torpid bat liver, linking it to coordinated nitrogen metabolism [PMID:bio_10.1101_2025.09.26.678923].

Mechanistic history

Synthesis pass · year-by-year structured walk · 9 steps
  1. 2014 High

    Whether the ADC/AGMAT route can substitute for the classical ODC1 polyamine pathway was unresolved; combined knockdown showed AGMAT provides a rescue route for putrescine synthesis supporting conceptus survival.

    Evidence In vivo morpholino knockdown of AGMAT and ODC1 with polyamine quantification in ovine conceptuses

    PMID:24648395

    Open questions at the time
    • Did not isolate AGMAT contribution independent of ODC1
    • Enzymatic activity on agmatine in this system not directly measured
  2. 2016 Medium

    It was unclear how agmatine signaling is regulated in mood circuits; AGMAT upregulation in PV/SST interneurons of CRTC1-null mice linked elevated AGMAT-mediated agmatine degradation to depressive-like behavior reversible by agmatine.

    Evidence Transcriptomics, qPCR/western blot, confocal immunofluorescence cell-type localization, and pharmacological rescue in Crtc1−/− mice

    PMID:27404284

    Open questions at the time
    • Causal role of AGMAT itself not tested by direct AGMAT manipulation
    • Mechanism linking eEF2 dephosphorylation to AGMAT activity not established
  3. 2017 High

    The developmental requirement for AGMAT was quantified; its knockdown caused abnormal, non-elongated conceptuses and reduced pregnancy, with compensatory upregulation of ADC and SLC22 transporters.

    Evidence In vivo morpholino knockdown with developmental phenotyping and mRNA expression analysis in ovine conceptuses

    PMID:29196820

    Open questions at the time
    • Compensatory transporter upregulation not mechanistically dissected
    • Combined ODC1 knockdown confounds AGMAT-specific attribution
  4. 2019 Medium

    How AGMAT promotes tumor growth was unknown; in lung adenocarcinoma it was shown to drive iNOS/NO-dependent MAPK and PI3K/Akt c-Myc activity and cyclin D1 induction.

    Evidence Gain/loss-of-function assays, NO detection, pharmacological inhibitors, and xenograft models

    PMID:31699997

    Open questions at the time
    • Link between AGMAT enzymatic activity and iNOS induction not defined
    • Single tumor lineage and single lab
  5. 2022 High

    The substrate identity of human AGMAT was redefined: it hydrolyzes linear guanidino acids rather than agmatine and lies downstream of GATM, prompting the proposed name guanidino acid hydrolase.

    Evidence In vitro enzymatic substrate profiling, structural modeling, and variant/mutagenesis analysis

    PMID:36543883

    Open questions at the time
    • In vivo relevance of guanidino acid hydrolysis versus polyamine-pathway roles not reconciled
    • Physiological tissue context of each variant not established
  6. 2022 Medium

    A second oncogenic mechanism was established in pancreatic cancer, where AGMAT activates TGFβ/Smad signaling and EMT to promote proliferation and metastasis.

    Evidence Gain/loss-of-function with proliferation, migration/invasion assays and TGFβ/Smad western blots

    PMID:35837051

    Open questions at the time
    • No mechanistic link between AGMAT metabolic output and TGFβ activation
    • Single lab, in vitro emphasis
  7. 2023 Medium

    Upstream regulation and downstream signaling of AGMAT in colorectal cancer were defined: c-Myc transcriptionally activates AGMAT, miR-151a-5p directly represses it, and AGMAT drives AKT/ERK signaling and tumor growth in vivo.

    Evidence Promoter-binding assays, dual luciferase reporter, AAV9-shRNA knockdown in AOM/DSS mouse model, and pathway western blots

    PMID:36680755 PMID:36704851

    Open questions at the time
    • Whether AGMAT acts via enzymatic product or non-enzymatic function in CRC unresolved
    • Direct biochemical demonstration of c-Myc occupancy in vivo limited
  8. 2025 Medium

    A stromal, non-cell-autonomous role emerged: tumor-derived exosomal miR-33a suppresses AGMAT in CAFs, lowering putrescine and remodeling KDM5C/H3K4me3/TIA1-dependent stress granule formation to aid cancer survival.

    Evidence Extracellular vesicle isolation, AGMAT targeting in CAFs, chromatin analysis, and stress granule assays

    PMID:40903826

    Open questions at the time
    • Direct enzymatic dependence on AGMAT for putrescine in CAFs not isolated from other polyamine enzymes
    • Single lab
  9. 2025 Medium

    A potential integration with urea-cycle nitrogen metabolism was identified through conserved physical association of AGMAT with CPS1 in torpid bat liver.

    Evidence Proteomics, confocal co-localization, and FRET across two bat species (preprint)

    PMID:bio_10.1101_2025.09.26.678923

    Open questions at the time
    • FRET indicates proximity not direct binding; no in vitro reconstitution
    • Functional consequence of the association not tested
    • Preprint, not peer-reviewed

Open questions

Synthesis pass · forward-looking unresolved questions
  • It remains unresolved how AGMAT's redefined guanidino acid hydrolase activity mechanistically connects to its polyamine-pathway, neuronal, and oncogenic roles, which are largely framed around agmatine/putrescine metabolism.
  • No study reconciles the in vitro substrate redefinition with in vivo agmatine-based models
  • Substrate flux measured in tumor, neuronal, and stromal contexts not directly determined

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0016740 transferase activity 2 GO:0016787 hydrolase activity 1
Pathway
R-HSA-1643685 Disease 5 R-HSA-1430728 Metabolism 3 R-HSA-162582 Signal Transduction 2
Partners

Evidence

Reading pass · 11 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2022 Human AGMAT (annotated as agmatinase) was shown biochemically to hydrolyze linear guanidino acids (taurocyamine, guanidinobutyrate, guanidinopropionate, guanidinoacetate) but was virtually inactive with agmatine as substrate. A negatively charged group at the end opposing the guanidine moiety was essential for catalysis. Two naturally occurring variants differ in substrate preferences. The authors propose renaming AGMAT as guanidino acid hydrolase (GDAH). Additionally, AGMAT substrates taurocyamine, guanidinobutyrate, and guanidinopropionate were shown to be produced by human glycine amidinotransferase (GATM), placing AGMAT downstream of GATM in guanidino acid metabolism. In vitro biochemical assays, structural modelling, direct substrate profiling, mutagenesis/variant analysis Scientific reports High 36543883
2025 In torpid bats, AGMAT co-localizes with carbamoyl-phosphate synthase 1 (CPS1) in liver, as demonstrated by proteomic analysis, confocal microscopy, and fluorescence resonance energy transfer (FRET), indicating a physical association (indirect interaction) between AGMAT and CPS1. This interaction was conserved across two phylogenetically distant bat species (Myotis ricketti and Rhinolophus ferrumequinum), suggesting AGMAT participates in coordinated nitrogen metabolism with the urea cycle during torpor. Proteomics, confocal co-localization microscopy, FRET bioRxivpreprint Medium bio_10.1101_2025.09.26.678923
2014 In vivo morpholino antisense knockdown of AGMAT (combined with ODC1 knockdown) in ovine conceptuses demonstrated that the ADC/AGMAT pathway (arginine → agmatine → putrescine) functions as a rescue/alternative polyamine biosynthesis route when the classical ODC1 pathway is compromised, supporting conceptus survival and development. In vivo morpholino antisense oligonucleotide knockdown, polyamine quantification, mRNA/protein analysis in ovine conceptuses Biology of reproduction High 24648395
2017 In vivo knockdown of AGMAT translation (combined with ODC1 knockdown) in ovine conceptuses resulted in 78% morphologically abnormal and non-elongated conceptuses and reduced pregnancy rate (22%), establishing that AGMAT is required for adequate polyamine synthesis and conceptus development during peri-implantation pregnancy. Compensation occurred through upregulation of ADC, SLC22A1, SLC22A2, and SLC22A3 mRNAs. In vivo morpholino antisense oligonucleotide knockdown, polyamine quantification, mRNA expression analysis, pregnancy outcome assessment Amino acids High 29196820
2019 AGMAT overexpression in lung adenocarcinoma cells promotes tumorigenesis by upregulating iNOS expression, thereby increasing nitric oxide (NO) release. Elevated NO activates MAPK and PI3K/Akt-dependent c-Myc activity, upregulating cyclin D1 and driving cell proliferation. This pathway was validated in vitro and in xenograft models using NO scavenger (Carboxy-PTIO), iNOS inhibitor (SMT), and confirmed by functional assays. Gain/loss-of-function cell assays, NO detection (DAF-FMDA probe, nitrite assay), pharmacological inhibitors, xenograft tumor model, western blot Cell death & disease Medium 31699997
2022 AGMAT overexpression in pancreatic adenocarcinoma cells activates the TGFβ/Smad signaling pathway and enhances epithelial-mesenchymal transition (EMT), promoting cell proliferation and metastasis, as shown by gain- and loss-of-function experiments with western blot pathway analysis. Gain/loss-of-function experiments, CCK-8 assay, colony formation, migration/invasion assays, western blot for TGFβ/Smad pathway components Experimental and therapeutic medicine Medium 35837051
2023 The oncogenic transcription factor c-Myc binds to the AGMAT promoter and transcriptionally upregulates AGMAT expression in colorectal cancer cells, as demonstrated by promoter-binding assays. AGMAT knockdown via AAV9-shRNA in a colitis-associated CRC mouse model reduced tumor number and size, decreased PCNA expression, and inhibited AKT and ERK phosphorylation, placing AGMAT upstream of PI3K/AKT and ERK signaling in CRC progression. Promoter-binding assay (c-Myc binding to AGMAT promoter), AAV9-shRNA knockdown in AOM/DSS mouse model, western blot for AKT/ERK phosphorylation, in vitro proliferation/apoptosis assays Human gene therapy Medium 36680755
2023 AGMAT was validated as a direct target of miR-151a-5p in colorectal carcinoma by dual luciferase reporter assay, establishing that miR-151a-5p suppresses AGMAT to promote CRC cell proliferation, migration, invasion, and epithelial-mesenchymal transition. Dual luciferase reporter assay, gain/loss-of-function cell assays for proliferation, migration, invasion Oncology reports Medium 36704851
2023 AGMAT overexpression in the ventral hippocampus of rats elicited depressive- and anxiety-like behaviors, whereas AGMAT knockdown in the same region had antidepressant and anxiolytic effects in chronic restraint stress animals. Electrophysiological recordings revealed that AGMAT blockade increased Schaffer collateral-CA1 excitatory synaptic transmission both pre- and post-synaptically, likely through inhibition of AGMAT-expressing local interneurons. Stereotaxic viral vector overexpression/knockdown in rat ventral hippocampus, behavioral testing, field and whole-cell electrophysiological recordings Neuropharmacology Medium 36849038
2016 Agmatinase (Agmat) is upregulated in the prefrontal cortex and hippocampus of CRTC1 knockout mice, and this upregulation is localized to parvalbumin- and somatostatin-positive interneurons, as confirmed by confocal immunofluorescence microscopy and qPCR/western blot. Acute agmatine treatment rescued the depressive-like behavior of Crtc1−/− mice, consistent with agmatine deficit due to elevated AGMAT-mediated degradation. Agmatine also decreased eEF2 phosphorylation in the PFC, suggesting NMDA receptor antagonist-like mechanism. Microarray gene expression profiling, qPCR, western blot, confocal immunofluorescence microscopy, behavioral testing (forced swim test), pharmacological agmatine/ketamine treatment Translational psychiatry Medium 27404284
2025 Exosomal miR-33a secreted by cancer cells targets AGMAT in cancer-associated fibroblasts (CAFs), suppressing putrescine biosynthesis. Reduced putrescine in CAFs inhibits KDM5C demethylase expression, altering H3K4me3 levels at the TIA1 locus and reducing stress granule (SG) formation in stromal CAFs, thereby supporting cancer cell survival under glucose starvation. Extracellular vesicle isolation, miR-33a overexpression/targeting of AGMAT in CAFs, KDM5C and H3K4me3 chromatin analysis, stress granule formation assays, ACO1 RNA-binding protein interaction studies Journal of extracellular vesicles Medium 40903826

Source papers

Stage 0 corpus · 33 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2023 Arginine reprograms metabolism in liver cancer via RBM39. Cell 226 37804830
2017 Physiological importance of polyamines. Zygote (Cambridge, England) 115 28587687
2014 Arginine decarboxylase and agmatinase: an alternative pathway for de novo biosynthesis of polyamines for development of mammalian conceptuses. Biology of reproduction 101 24648395
2016 The Dysregulation of Polyamine Metabolism in Colorectal Cancer Is Associated with Overexpression of c-Myc and C/EBPβ rather than Enterotoxigenic Bacteroides fragilis Infection. Oxidative medicine and cellular longevity 75 27433286
2016 Involvement of the agmatinergic system in the depressive-like phenotype of the Crtc1 knockout mouse model of depression. Translational psychiatry 50 27404284
2019 Agmatinase promotes the lung adenocarcinoma tumorigenesis by activating the NO-MAPKs-PI3K/Akt pathway. Cell death & disease 31 31699997
2021 Pre-implantation exogenous progesterone and pregnancy in sheep. II. Effects on fetal-placental development and nutrient transporters in late pregnancy. Journal of animal science and biotechnology 28 33827696
2025 Single-cell and spatial-resolved profiling reveals cancer-associated fibroblast heterogeneity in colorectal cancer metabolic subtypes. Journal of translational medicine 26 39934919
2017 De novo sequencing and comparative analysis of testicular transcriptome from different reproductive phases in freshwater spotted snakehead Channa punctatus. PloS one 24 28253373
2024 Genetic imputation of kidney transcriptome, proteome and multi-omics illuminates new blood pressure and hypertension targets. Nature communications 18 38504097
2018 Effects of catecholamines on secretion of interferon tau and expression of genes for synthesis of polyamines and apoptosis by ovine trophectoderm. Biology of reproduction 17 29668843
2020 Genome-wide scan identifies novel genetic loci regulating salivary metabolite levels. Human molecular genetics 16 31960908
2018 Functional roles of ornithine decarboxylase and arginine decarboxylase during the peri-implantation period of pregnancy in sheep. Journal of animal science and biotechnology 15 29410783
2023 miR‑151a‑5p promotes the proliferation and metastasis of colorectal carcinoma cells by targeting AGMAT. Oncology reports 12 36704851
2022 Polygenic risk score trend and new variants on chromosome 1 are associated with male gout in genome-wide association study. Arthritis research & therapy 11 36221101
2024 Multi-Omic Analysis of Esophageal Adenocarcinoma Uncovers Candidate Therapeutic Targets and Cancer-Selective Posttranscriptional Regulation. Molecular & cellular proteomics : MCP 9 38604503
2017 Functional roles of agmatinase during the peri-implantation period of pregnancy in sheep. Amino acids 8 29196820
2023 The expression of agmatinase manipulates the affective state of rats subjected to chronic restraint stress. Neuropharmacology 7 36849038
2022 Guanidino acid hydrolysis by the human enzyme annotated as agmatinase. Scientific reports 7 36543883
2018 Effects of Bisphenol-A on proliferation and expression of genes related to synthesis of polyamines, interferon tau and insulin-like growth factor 2 by ovine trophectoderm cells. Reproductive toxicology (Elmsford, N.Y.) 7 29635046
2024 Comparative transcriptome profile of embryos at different developmental stages derived from somatic cell nuclear transfer (SCNT) and in-vitro fertilization (IVF) in riverine buffalo (Bubalus bubalis). Veterinary research communications 6 38829518
2024 Identification and experimental validation of key genes in osteoarthritis based on machine learning algorithms and single-cell sequencing analysis. Heliyon 6 39286216
2022 Agmatinase facilitates the tumorigenesis of pancreatic adenocarcinoma through the TGFβ/Smad pathway. Experimental and therapeutic medicine 6 35837051
2024 Subtype-specific transcription factors affect polyamine metabolism and the tumor microenvironment in breast cancer. Cancer innovation 5 39629335
2015 Potential biomarkers associated with diabetic glomerulopathy through proteomics. Renal failure 5 26364511
2025 Integrated single-cell transcriptomic map of pig kidney cells across various periods and anatomical sites. Zoological research 4 40116025
2025 Cancer Cell-Secreted miR-33a Reduces Stress Granule Formation by Targeting Polyamine Metabolism in Stroma to Promote Tumourigenesis. Journal of extracellular vesicles 4 40903826
2025 Comprehensive analysis of cuproptosis and m6A-Target gene signatures for diagnostic significance and immune microenvironment characterization in polycystic ovary syndrome. Scientific reports 3 40481029
2024 Integrated histopathology and transcriptome metabolome profiling reveal the toxicity mechanism of phenazine-1-carboxylic acid in zebrafish. Environmental pollution (Barking, Essex : 1987) 3 38272164
2023 Adeno-Associated Virus-Mediated Knockdown of Agmatinase Attenuates Inflammation and Tumorigenesis in a Mouse Model of Colitis-Associated Colorectal Cancer. Human gene therapy 3 36680755
2023 Predicting Survival Signature of Bladder Cancer Related to Cancer-Associated Fibroblast (CAF) Constructed by Intersecting Genes in TCGA and GEO. Molecular biotechnology 3 37749482
2026 Multiomics analysis of polyamine metabolism in colorectal cancer, highlighting the key role of extracellular putrescine in impairing CXCR6+CD8+ T cell anti-tumor activity. PeerJ 0 41700134
2026 Increased Agmatine Degradation in Children with Specific Learning Disorder. International journal of molecular sciences 0 41977269

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