General Information of Drug-Metabolizing Enzyme (DME) (ID: DE1ZNSC)

DME Name Heparanase (HPSE)
Synonyms Endo-glucoronidase; Heparanase 50 kDa subunit; Heparanase 8 kDa subunit; Heparanase-1; HEP; HPA; HPA1; Hpa1; HPR1; HPSE; HPSE1; HSE1
Gene Name HPSE
UniProt ID
HPSE_HUMAN
INTEDE ID
DME0113
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
10855
EC Number EC: 3.2.1.166
Hydrolases
Glycosylase
O/S-glycosyl compound glycosidase
EC: 3.2.1.166
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MLLRSKPALPPPLMLLLLGPLGPLSPGALPRPAQAQDVVDLDFFTQEPLHLVSPSFLSVT
IDANLATDPRFLILLGSPKLRTLARGLSPAYLRFGGTKTDFLIFDPKKESTFEERSYWQS
QVNQDICKYGSIPPDVEEKLRLEWPYQEQLLLREHYQKKFKNSTYSRSSVDVLYTFANCS
GLDLIFGLNALLRTADLQWNSSNAQLLLDYCSSKGYNISWELGNEPNSFLKKADIFINGS
QLGEDFIQLHKLLRKSTFKNAKLYGPDVGQPRRKTAKMLKSFLKAGGEVIDSVTWHHYYL
NGRTATKEDFLNPDVLDIFISSVQKVFQVVESTRPGKKVWLGETSSAYGGGAPLLSDTFA
AGFMWLDKLGLSARMGIEVVMRQVFFGAGNYHLVDENFDPLPDYWLSLLFKKLVGTKVLM
ASVQGSKRRKLRVYLHCTNTDNPRYKEGDLTLYAINLHNVTKYLRLPYPFSNKQVDKYLL
RPLGPHGLLSKSVQLNGLTLKMVDDQTLPPLMEKPLRPGSSLGLPAFSYSFFVIRNAKVA
ACI
Function
This enzyme cleaves heparan sulfate proteoglycans (HSPGs) into heparan sulfate side chains and core proteoglycans. It selectively cleaves the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying either a 3-O-sulfo or a 6-O-sulfo group. It can also cleave the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying a 2-O-sulfo group, but not linkages between a glucuronic acid unit and a 2-O-sulfated iduronic acid moiety.
KEGG Pathway
Glycosaminoglycan degradation (hsa00531 )
Metabolic pathways (hsa01100 )
Proteoglycans in cancer (hsa05205 )
Reactome Pathway
Neutrophil degranulation (R-HSA-6798695 )
HS-GAG degradation (R-HSA-2024096 )

Molecular Expression Atlas (MEA) of This DME

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DME
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2B33.1 Bone marrow 1.38E-09 -6.83E-01 -8.14E-01
Alopecia ED70 Skin from scalp 6.46E-02 2.51E-01 3.23E-01
Alzheimer's disease 8A20 Entorhinal cortex 2.56E-06 2.41E-01 8.27E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 4.69E-01 4.91E-02 1.02E-01
Aortic stenosis BB70 Calcified aortic valve 9.56E-02 7.82E-01 1.43E+00
Apnea 7A40 Hyperplastic tonsil 2.68E-01 -6.77E-01 -1.26E+00
Arthropathy FA00-FA5Z Peripheral blood 1.45E-02 3.06E-01 7.81E-01
Asthma CA23 Nasal and bronchial airway 5.99E-07 7.73E-01 5.96E-01
Atopic dermatitis EA80 Skin 4.53E-01 -4.21E-01 -1.56E+00
Autism 6A02 Whole blood 3.83E-01 4.48E-02 8.94E-02
Autoimmune uveitis 9A96 Peripheral monocyte 6.30E-02 4.17E-01 2.69E-01
Autosomal dominant monocytopenia 4B04 Whole blood 6.15E-02 1.59E+00 2.88E+00
Bacterial infection of gingival 1C1H Gingival tissue 8.54E-16 -5.54E-01 -1.54E+00
Batten disease 5C56.1 Whole blood 7.55E-01 1.14E-01 2.02E-01
Behcet's disease 4A62 Peripheral blood 9.34E-01 -1.59E-01 -3.35E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 1.30E-01 -9.21E-02 -4.80E-01
Bladder cancer 2C94 Bladder tissue 8.72E-06 2.97E-01 1.32E+00
Breast cancer 2C60-2C6Z Breast tissue 6.31E-57 5.71E-01 1.24E+00
Cardioembolic stroke 8B11.20 Whole blood 1.08E-07 5.76E-01 1.44E+00
Cervical cancer 2C77 Cervical tissue 5.72E-01 -2.27E-01 -4.01E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 5.07E-01 2.40E-01 2.73E-01
Chronic hepatitis C 1E51.1 Whole blood 7.69E-01 -3.37E-01 -3.23E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 1.51E-01 -5.44E-02 -1.28E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 3.06E-02 -1.56E-01 -3.38E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 5.11E-01 1.44E-01 4.35E-01
Colon cancer 2B90 Colon tissue 8.18E-47 -7.15E-01 -1.75E+00
Coronary artery disease BA80-BA8Z Peripheral blood 7.42E-01 1.06E-01 2.00E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 7.94E-01 -1.21E-01 -1.79E-01
Endometriosis GA10 Endometrium tissue 9.03E-04 6.22E-01 9.63E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 7.15E-01 2.05E-01 8.26E-01
Familial hypercholesterolemia 5C80.00 Whole blood 5.24E-16 1.17E+00 1.78E+00
Gastric cancer 2B72 Gastric tissue 5.02E-02 1.77E+00 2.53E+00
Glioblastopma 2A00.00 Nervous tissue 2.78E-89 6.30E-01 1.54E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 1.68E-01 -9.52E-01 -2.22E+00
Glioma 2A00.0Y-2A00.0Z White matter tissue 8.03E-02 5.49E-01 3.71E-01
Head and neck cancer 2D42 Head and neck tissue 5.19E-02 2.38E-01 2.78E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 2.54E-01 7.72E-02 3.31E-01
Huntington's disease 8A01.10 Whole blood 7.38E-01 -3.09E-01 -3.93E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 4.14E-01 -2.02E-01 -5.02E-01
Immunodeficiency 4A00-4A20 Peripheral blood 2.64E-04 4.70E-01 1.94E+00
Influenza 1E30 Whole blood 9.91E-01 4.44E-01 4.94E-01
Interstitial cystitis GC00.3 Bladder tissue 3.14E-06 1.02E+00 7.62E+00
Intracranial aneurysm 8B01.0 Intracranial artery 4.73E-02 6.88E-01 2.06E+00
Irritable bowel syndrome DD91.0 Rectal colon tissue 6.86E-01 -1.02E-02 -2.68E-02
Ischemic stroke 8B11 Peripheral blood 8.27E-01 1.94E-01 5.14E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 8.12E-05 2.90E-01 4.92E-01
Lateral sclerosis 8B60.4 Skin 5.05E-01 1.70E-01 3.05E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 3.78E-03 4.20E-01 2.08E+00
Liver cancer 2C12.0 Liver tissue 1.18E-01 -1.85E-01 -3.04E-01
Liver failure DB99.7-DB99.8 Liver tissue 1.41E-04 1.74E+00 2.54E+00
Lung cancer 2C25 Lung tissue 1.42E-47 8.66E-01 1.62E+00
Lupus erythematosus 4A40 Whole blood 5.11E-01 1.98E-01 1.55E-01
Major depressive disorder 6A70-6A7Z Hippocampus 8.08E-01 -2.21E-02 -1.27E-01
Major depressive disorder 6A70-6A7Z Whole blood 8.77E-02 2.17E-01 5.45E-01
Melanoma 2C30 Skin 7.77E-04 1.02E+00 8.87E-01
Multiple myeloma 2A83.1 Peripheral blood 5.03E-01 6.16E-02 6.75E-02
Multiple myeloma 2A83.1 Bone marrow 2.21E-02 2.38E-01 6.42E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 1.39E-01 3.92E-01 6.05E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 6.63E-08 4.32E-01 9.25E-01
Myelofibrosis 2A20.2 Whole blood 7.18E-03 8.89E-01 2.80E+00
Myocardial infarction BA41-BA50 Peripheral blood 2.30E-02 8.15E-01 8.37E-01
Myopathy 8C70.6 Muscle tissue 2.21E-05 4.81E-01 5.63E+00
Neonatal sepsis KA60 Whole blood 1.32E-21 1.06E+00 1.45E+00
Neuroectodermal tumour 2A00.11 Brain stem tissue 2.45E-01 -2.30E-01 -5.87E-01
Non-alcoholic fatty liver disease DB92 Liver tissue 3.45E-02 4.41E-01 2.05E+00
Obesity related type 2 diabetes 5A11 Omental adipose tissue 7.15E-02 -5.45E-01 -1.03E+00
Olive pollen allergy CA08.00 Peripheral blood 3.34E-02 -6.95E-01 -1.20E+00
Oral cancer 2B6E Oral tissue 9.48E-01 -2.46E-01 -2.13E-01
Osteoarthritis FA00-FA0Z Synovial tissue 1.22E-02 8.41E-01 1.29E+00
Osteoporosis FB83.1 Bone marrow 4.63E-01 7.48E-02 1.19E-01
Ovarian cancer 2C73 Ovarian tissue 2.20E-03 6.75E-01 1.42E+00
Pancreatic cancer 2C10 Pancreas 3.04E-05 8.04E-01 1.53E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 5.08E-01 -2.90E-02 -1.09E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 1.02E-05 1.25E+00 1.44E+00
Pituitary cancer 2D12 Pituitary tissue 4.42E-01 9.77E-02 2.19E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 6.51E-01 2.38E-01 5.11E-01
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 7.85E-01 5.57E-02 3.12E-01
Polycythemia vera 2A20.4 Whole blood 2.01E-14 7.96E-01 2.31E+00
Pompe disease 5C51.3 Biceps muscle 1.13E-02 3.85E-01 2.42E+00
Preterm birth KA21.4Z Myometrium 2.93E-01 -8.00E-01 -1.05E+00
Prostate cancer 2C82 Prostate 8.10E-01 1.89E-01 2.26E-01
Psoriasis EA90 Skin 9.55E-64 2.83E+00 5.16E+00
Rectal cancer 2B92 Rectal colon tissue 4.68E-05 -1.08E+00 -3.83E+00
Renal cancer 2C90-2C91 Kidney 8.04E-07 9.28E-01 2.43E+00
Retinoblastoma 2D02.2 Uvea 1.82E-04 1.74E+00 2.98E+01
Rheumatoid arthritis FA20 Synovial tissue 3.54E-02 5.10E-01 8.01E-01
Rhinovirus infection CA42.1 Nasal epithelium tissue 2.11E-01 1.31E-01 2.69E-01
Schizophrenia 6A20 Prefrontal cortex 8.01E-02 7.01E-02 4.25E-02
Schizophrenia 6A20 Superior temporal cortex 8.62E-01 -5.05E-02 -3.93E-01
Scleroderma 4A42.Z Whole blood 7.77E-03 2.20E-01 8.13E-01
Seizure 8A60-8A6Z Whole blood 7.06E-01 -1.34E-01 -1.45E-01
Sensitive skin EK0Z Skin 3.05E-01 3.44E-01 9.11E-01
Sepsis with septic shock 1G41 Whole blood 8.58E-56 1.33E+00 1.85E+00
Shwachman-Diamond syndrome 3A70.0 Bone marrow 7.07E-01 -1.01E-01 -4.22E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 2.68E-06 2.48E+00 3.78E+00
Simpson golabi behmel syndrome LD2C Adipose tissue 9.16E-01 1.11E-01 5.56E-01
Sjogren's syndrome 4A43.2 Salivary gland tissue 2.15E-01 -4.35E-01 -1.18E+00
Skin cancer 2C30-2C3Z Skin 1.19E-02 1.47E-01 2.34E-01
Thrombocythemia 3B63 Whole blood 2.07E-02 3.83E-01 1.20E+00
Thrombocytopenia 3B64 Whole blood 4.91E-02 -4.93E-01 -6.42E-01
Thyroid cancer 2D10 Thyroid 1.12E-22 8.07E-01 1.39E+00
Tibial muscular dystrophy 8C75 Muscle tissue 3.94E-05 5.26E-01 2.17E+00
Tuberous sclerosis complex LD2D.2 Perituberal tissue 1.16E-01 5.60E-01 3.90E+00
Type 2 diabetes 5A11 Liver tissue 3.86E-01 4.25E-02 1.38E-01
Ureter cancer 2C92 Urothelium 8.90E-01 4.33E-02 9.29E-02
Uterine cancer 2C78 Endometrium tissue 4.23E-02 5.24E-01 4.40E-01
Vitiligo ED63.0 Skin 9.76E-01 -1.82E-01 -3.19E-01
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⏷ Show the Full List of DME Expression Under 107 Diseases

The Drug Therapeutic Target (DTT) Role of This DME

DME DTT Name Heparanase (HPSE) DTT Info
DME DTT Type Successful
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PG-545 DM68D3O Ocular disease 1F00.1Z Phase 1 [1]
Suramin DMTOUY9 African trypanosomiasis 1F51 Phase 1 [2]
1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Neutralase DMXHWK6 Angiogenesis disorder BE2Z Discontinued in Phase 3 [3]

References

1 PG545, a dual heparanase and angiogenesis inhibitor, induces potent anti-tumour and anti-metastatic efficacy in preclinical models. Br J Cancer. 2011 Feb 15;104(4):635-42.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1728).
3 Heparanase neutralizes the anticoagulation properties of heparin and low-molecular-weight heparin. J Thromb Haemost. 2006 Mar;4(3):560-5.