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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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METAP2
methionyl aminopeptidase 2
Chromosome 12 · 12q22
NCBI Gene: 10988Ensembl: ENSG00000111142.14HGNC: HGNC:16672UniProt: A0A140VJE3
113PubMed Papers
20Diseases
3Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Protease
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
protein bindingprotein processingcytoplasmcytosolneurodegenerative diseaseneuroinflammatory disorderobesitypreeclampsia
✦AI Summary

METAP2 (methionyl aminopeptidase 2) is a metalloprotease that removes N-terminal methionine residues from nascent proteins, playing a critical role in protein synthesis regulation 1. Beyond its canonical aminopeptidase function, METAP2 protects eukaryotic initiation factor EIF2S1 from translation-inhibiting phosphorylation and regulates lipid metabolism and energy balance 1. METAP2 serves as a cytoplasmic shuttle protein in targeted protein relocalization mechanisms, facilitating redistribution of disease-associated proteins to alter cellular interactomes 2. In cancer biology, METAP2 is upregulated in ovarian cancer where it stabilizes the RNA-binding protein YTHDF2 by attenuating K48-linked ubiquitination, promoting cancer cell proliferation and migration through altered mRNA decay of tumor suppressors 3. Therapeutically, METAP2 inhibitors including fumagillin, TNP-470, beloranib, and ZGN-1061 show promise across multiple disease contexts 1. Recent evidence demonstrates METAP2 inhibitor BL6 reduces neuroinflammation in microglia and Alzheimer's disease models by suppressing pro-inflammatory cytokines and promoting microglial polarization 4. Additionally, MetAP2 is an essential survival factor in microsporidian parasites and represents a validated antimicrobial drug target 5. These diverse functions position METAP2 as a pleiotropic therapeutic target for metabolic, oncologic, and neurodegenerative diseases.

Sources cited
1
METAP2 structure, catalytic mechanism, and role in regulating lipid metabolism, energy balance, and protein synthesis; multiple inhibitor development and mechanisms
PMID: 39766279
2
METAP2 functions as a cytoplasmic shuttle protein for targeted protein relocalization and interactome rewiring in disease contexts
PMID: 39294374
3
METAP2 upregulation in ovarian cancer; stabilizes YTHDF2 via attenuation of K48-linked ubiquitination; promotes cancer progression and clinical value of ZGN-1061 inhibitor
PMID: 41102384
4
METAP2 inhibitor BL6 reduces neuroinflammation, suppresses pro-inflammatory cytokines, and promotes microglial M1 to M2 polarization in Alzheimer's disease models
PMID: 39942725
5
MetAP2 is essential gene for Nosema bombycis survival and validated target for antimicrobial drug fumagillin
PMID: 30175023
6
METAP2 identified as RNA-binding protein with cytoplasmic functions involved in gene regulation
PMID: 39325823
Disease Associationsⓘ20
neurodegenerative diseaseOpen Targets
0.52Moderate
neuroinflammatory disorderOpen Targets
0.32Weak
obesityOpen Targets
0.30Weak
preeclampsiaOpen Targets
0.28Weak
Prader-Willi syndromeOpen Targets
0.26Weak
type 2 diabetes mellitusOpen Targets
0.21Weak
myelodysplastic syndromeOpen Targets
0.10Suggestive
acute myeloid leukemiaOpen Targets
0.10Suggestive
sialolithiasisOpen Targets
0.09Suggestive
acute myeloid leukemia by FAB classificationOpen Targets
0.07Suggestive
breast cancerOpen Targets
0.06Suggestive
neoplasmOpen Targets
0.06Suggestive
cancerOpen Targets
0.04Suggestive
hepatocellular carcinomaOpen Targets
0.03Suggestive
cholangiocarcinomaOpen Targets
0.03Suggestive
Netherton syndromeOpen Targets
0.03Suggestive
mesotheliomaOpen Targets
0.03Suggestive
ovarian cancerOpen Targets
0.02Suggestive
pachyonychia congenitaOpen Targets
0.02Suggestive
chronic granulomatous diseaseOpen Targets
0.02Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets3
ACLIMOSTATPhase II
Methionine aminopeptidase 2 inhibitor
type 2 diabetes mellitus
BELORANIBPhase III
Methionine aminopeptidase 2 inhibitor
TOSEDOSTATPhase II
Aminopeptidase inhibitor
acute myeloid leukemia by FAB classification
Related Genes
CUL7Protein interaction100%RPL4Protein interaction100%RPS5Protein interaction100%MRPL36Protein interaction100%MRPS6Protein interaction100%RPS2Protein interaction100%
Tissue Expression6 tissues
Bone Marrow
100%
Heart
73%
Brain
54%
Liver
49%
Ovary
44%
Lung
38%
Gene Interaction Network
Click a node to explore
METAP2CUL7RPL4RPS5MRPL36MRPS6RPS2
PROTEIN STRUCTURE
Preparing viewer…
PDB5D6E · 1.49 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.75LoF Tolerant
pLIⓘ
0.05Tolerant
Observed/Expected LoF0.47 [0.31–0.75]
RankingsWhere METAP2 stands among ~20K protein-coding genes
  • #4,192of 20,598
    Most Researched113 · top quartile
  • #5,996of 17,882
    Most Constrained (LOEUF)0.75
Genes detectedMETAP2
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Targeted protein relocalization via protein transport coupling.
PMID: 39294374
Nature · 2024
1.00
2
Protacs: chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation.
PMID: 11438690
Proc Natl Acad Sci U S A · 2001
0.90
3
Molecular characterization and phylogenetic analyses of MetAP2 gene and protein of
PMID: 39005720
Front Vet Sci · 2024
0.80
4
MetAP2 as a Therapeutic Target for Obesity and Type 2 Diabetes: Structural Insights, Mechanistic Roles, and Inhibitor Development.
PMID: 39766279
Biomolecules · 2024
0.70
5
Human cells contain myriad excised linear intron RNAs with links to gene regulation and potential utility as biomarkers.
PMID: 39325823
PLoS Genet · 2024
0.60