Details of Drug-Metabolizing Enzyme (DME)

General Information of Drug-Metabolizing Enzyme (DME) (ID: DE6TFXV)

DME Name Tyrosine-protein phosphatase non-receptor 1 (PTP1B)
Synonyms Tyrosine-protein phosphatase non-receptor type 1; Protein-tyrosine phosphatase 1B; PTP-1B; PTP1B; PTPN1
Gene Name PTPN1
UniProt ID
PTN1_HUMAN
INTEDE ID
DME0495
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Gene ID
5770
EC Number EC: 3.1.3.48
Hydrolases
Ester bond hydrolase
Phosphoric monoester hydrolase
EC: 3.1.3.48
Lineage Species: Homo sapiens
Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Primates
Family: Hominidae
Genus: Homo
Species: Homo sapiens
Sequence
MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLH
QEDNDYINASLIKMEEAQRSYILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLK
CAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLELENLTTQETREILHFHYTTWP
DFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD
PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLE
PPPEHIPPPPRPPKRILEPHNGKCREFFPNHQWVKEETQEDKDCPIKEEKGSPLNAAPYG
IESMSQDTEVRSRVVGGSLRGAQAASPAKGEPSLPEKDEDHALSYWKPFLVNMCVATVLT
AGAYLCYRFLFNSNT
Function This enzyme mediates dephosphorylation of EIF2AK3/PERK and inactivates the protein kinase activity of EIF2AK3/PERK.
KEGG Pathway
Adherens junction (hsa04520 )
Insulin resistance (hsa04931 )
Insulin signaling pathway (hsa04910 )
Reactome Pathway
Integrin alphaIIb beta3 signaling (R-HSA-354192 )
MECP2 regulates neuronal receptors and channels (R-HSA-9022699 )
Negative regulation of MET activity (R-HSA-6807004 )
PTK6 Down-Regulation (R-HSA-8849472 )
Regulation of IFNA signaling (R-HSA-912694 )
Regulation of IFNG signaling (R-HSA-877312 )
Growth hormone receptor signaling (R-HSA-982772 )

Molecular Interaction Atlas (MIA) of This DME

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DME
1 Investigative Drug(s) Metabolized by This DME
Drug Name Drug ID Indication ICD 11 Highest Status REF
4-nitrophenyl phosphate DMBX4UJ Discovery agent N.A. Investigative [5]
Experimental Enzyme Kinetic Data of Drugs
Drug Name Indication Highest Status Kinetic Data REF
4-nitrophenyl phosphate Discovery agent [N.A.] Investigative Km = 0.38 microM [5]

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 4.96E-02 3.77E-02 2.81E-01
Alopecia ED70 Skin from scalp 8.00E-01 -9.75E-03 -5.00E-02
Alzheimer's disease 8A20 Entorhinal cortex 3.61E-01 -1.78E-02 -1.39E-01
Ankylosing spondylitis FA92.0 Pheripheral blood 1.00E-01 1.72E-01 1.00E+00
Aortic stenosis BB70 Calcified aortic valve 8.05E-01 1.12E-01 2.39E-01
Apnea 7A40 Hyperplastic tonsil 5.48E-01 4.36E-02 2.82E-01
Arthropathy FA00-FA5Z Peripheral blood 5.72E-01 8.64E-02 5.11E-01
Asthma CA23 Nasal and bronchial airway 2.53E-06 -1.66E-01 -3.37E-01
Atopic dermatitis EA80 Skin 7.28E-03 -6.29E-02 -6.95E-01
Autism 6A02 Whole blood 8.65E-01 -6.43E-03 -3.68E-02
Autoimmune uveitis 9A96 Peripheral monocyte 9.43E-02 -2.47E-01 -2.28E+00
Autosomal dominant monocytopenia 4B04 Whole blood 1.67E-01 2.56E-04 1.10E-03
Bacterial infection of gingival 1C1H Gingival tissue 5.08E-06 9.17E-02 5.96E-01
Batten disease 5C56.1 Whole blood 2.43E-01 4.98E-02 6.08E-01
Behcet's disease 4A62 Peripheral blood 4.47E-01 -2.21E-02 -1.25E-01
Bipolar disorder 6A60-6A6Z Prefrontal cortex 2.71E-01 -4.72E-02 -3.17E-01
Bladder cancer 2C94 Bladder tissue 4.33E-04 3.39E-01 2.42E+00
Breast cancer 2C60-2C6Z Breast tissue 1.51E-03 2.25E-02 1.26E-01
Cardioembolic stroke 8B11.20 Whole blood 1.08E-02 -1.44E-01 -6.38E-01
Cervical cancer 2C77 Cervical tissue 6.07E-01 5.16E-02 2.51E-01
Childhood onset rheumatic disease FA20.Z Peripheral blood 3.80E-01 3.69E-02 1.93E-01
Chronic hepatitis C 1E51.1 Whole blood 2.23E-01 9.05E-02 5.98E-01
Chronic obstructive pulmonary disease CA22 Lung tissue 5.24E-01 7.89E-02 3.33E-01
Chronic obstructive pulmonary disease CA22 Small airway epithelium 1.36E-02 6.16E-02 5.08E-01
Chronic rhinosinusitis CA0A Sinus mucosa tissue 9.74E-01 1.80E-02 1.83E-01
Colon cancer 2B90 Colon tissue 7.56E-08 -7.08E-02 -4.05E-01
Coronary artery disease BA80-BA8Z Peripheral blood 8.25E-01 7.38E-02 3.52E-01
Diffuse large B-cell lymphoma 2A81 Tonsil tissue 1.65E-01 -6.72E-02 -3.90E-01
Endometriosis GA10 Endometrium tissue 5.98E-01 5.29E-02 3.79E-01
Familial hypercholesterolemia 5C80.00 Peripheral blood 7.34E-02 -9.54E-02 -9.52E-01
Familial hypercholesterolemia 5C80.00 Whole blood 5.88E-01 4.95E-03 3.79E-02
Gastric cancer 2B72 Gastric tissue 5.62E-01 -1.16E-01 -5.95E-01
Glioblastopma 2A00.00 Nervous tissue 3.54E-62 -2.15E-01 -1.13E+00
Glioma 2A00.0Y-2A00.0Z Brain stem tissue 8.85E-01 -2.20E-02 -9.57E-01
Glioma 2A00.0Y-2A00.0Z White matter tissue 7.74E-01 8.24E-02 3.74E-01
Head and neck cancer 2D42 Head and neck tissue 4.15E-01 -1.94E-02 -1.49E-01
HIV-associated neurocognitive impairment 8A2Y-8A2Z White matter tissue 1.25E-01 -7.60E-02 -2.74E-01
Huntington's disease 8A01.10 Whole blood 7.45E-01 -4.60E-02 -2.96E-01
Idiopathic pulmonary fibrosis CB03.4 Lung tissue 8.92E-02 -3.83E-01 -9.70E-01
Immunodeficiency 4A00-4A20 Peripheral blood 7.37E-02 6.14E-02 7.50E-01
Influenza 1E30 Whole blood 9.39E-01 1.20E-01 5.55E-01
Interstitial cystitis GC00.3 Bladder tissue 1.28E-01 1.14E-01 1.06E+00
Intracranial aneurysm 8B01.0 Intracranial artery 7.20E-01 -5.59E-02 -3.77E-01
Irritable bowel syndrome DD91.0 Rectal colon tissue 6.81E-01 -2.56E-02 -1.43E-01
Ischemic stroke 8B11 Peripheral blood 7.31E-01 5.86E-02 4.61E-01
Juvenile idiopathic arthritis FA24 Peripheral blood 2.61E-02 6.19E-02 1.47E-01
Lateral sclerosis 8B60.4 Skin 6.47E-01 3.58E-02 4.33E-01
Lateral sclerosis 8B60.4 Cervical spinal cord 6.08E-01 -6.46E-02 -2.76E-01
Liver cancer 2C12.0 Liver tissue 7.82E-08 -1.60E-01 -1.02E+00
Liver failure DB99.7-DB99.8 Liver tissue 2.39E-01 -1.18E-01 -6.42E-01
Lung cancer 2C25 Lung tissue 1.50E-16 -1.72E-01 -7.02E-01
Lupus erythematosus 4A40 Whole blood 1.77E-01 -1.32E-03 -6.24E-03
Major depressive disorder 6A70-6A7Z Hippocampus 5.44E-01 -1.80E-02 -1.32E-01
Major depressive disorder 6A70-6A7Z Whole blood 9.44E-01 2.07E-02 1.11E-01
Melanoma 2C30 Skin 1.29E-01 2.44E-01 5.56E-01
Multiple myeloma 2A83.1 Peripheral blood 9.33E-01 3.92E-02 2.69E-01
Multiple myeloma 2A83.1 Bone marrow 2.20E-03 7.39E-02 9.74E-01
Multiple sclerosis 8A40 Plasmacytoid dendritic cells 1.36E-01 8.35E-02 2.74E-01
Myelodysplastic syndrome 2A36-2A3Z Bone marrow 8.11E-01 -2.76E-02 -2.73E-01
Myelofibrosis 2A20.2 Whole blood 1.84E-01 -1.19E-02 -1.56E-01
Myocardial infarction BA41-BA50 Peripheral blood 9.96E-02 6.38E-02 1.47E-01
Myopathy 8C70.6 Muscle tissue 1.31E-02 -1.77E-01 -1.00E+00
Neonatal sepsis KA60 Whole blood 3.11E-05 7.12E-02 4.92E-01
Neuroectodermal tumour 2A00.11 Brain stem tissue 2.57E-04 -5.09E-01 -2.10E+00
Non-alcoholic fatty liver disease DB92 Liver tissue 7.09E-01 4.96E-02 2.35E-01
Obesity related type 2 diabetes 5A11 Omental adipose tissue 2.39E-01 5.30E-02 3.85E-01
Olive pollen allergy CA08.00 Peripheral blood 8.46E-01 4.18E-02 1.61E-01
Oral cancer 2B6E Oral tissue 2.33E-02 -1.26E-01 -6.14E-01
Osteoarthritis FA00-FA0Z Synovial tissue 1.26E-01 -7.13E-02 -5.19E-01
Osteoporosis FB83.1 Bone marrow 1.40E-01 2.65E-01 4.90E+00
Ovarian cancer 2C73 Ovarian tissue 1.28E-01 -1.45E-01 -7.76E-01
Pancreatic cancer 2C10 Pancreas 5.28E-04 -2.82E-01 -1.33E+00
Parkinson's disease 8A00.0 Substantia nigra tissue 7.55E-01 5.90E-02 3.29E-01
Pediatric respiratory syncytial virus infection CA40.11 Peripheral blood 1.84E-02 5.39E-02 5.40E-01
Pituitary cancer 2D12 Pituitary tissue 1.47E-01 6.71E-02 4.02E-01
Pituitary gonadotrope tumour 2D12 Pituitary tissue 9.22E-01 -7.62E-03 -4.14E-02
Polycystic ovary syndrome 5A80.1 Vastus lateralis muscle 6.78E-02 -7.89E-02 -6.18E-01
Polycythemia vera 2A20.4 Whole blood 8.30E-02 4.60E-02 6.00E-01
Pompe disease 5C51.3 Biceps muscle 4.70E-01 -4.98E-02 -1.98E-01
Preterm birth KA21.4Z Myometrium 3.79E-01 -1.31E-02 -1.42E-01
Prostate cancer 2C82 Prostate 2.00E-01 4.73E-02 1.56E-01
Psoriasis EA90 Skin 8.28E-02 -4.82E-02 -2.07E-01
Rectal cancer 2B92 Rectal colon tissue 5.47E-01 -4.55E-02 -2.72E-01
Renal cancer 2C90-2C91 Kidney 4.31E-03 -3.77E-01 -1.33E+00
Retinoblastoma 2D02.2 Uvea 6.66E-01 3.15E-02 3.37E-01
Rheumatoid arthritis FA20 Synovial tissue 3.75E-02 -2.57E-01 -1.20E+00
Rhinovirus infection CA42.1 Nasal epithelium tissue 1.88E-01 1.71E-02 2.03E-01
Schizophrenia 6A20 Prefrontal cortex 6.82E-01 -4.19E-04 -3.41E-03
Schizophrenia 6A20 Superior temporal cortex 5.63E-01 4.77E-02 5.76E-01
Scleroderma 4A42.Z Whole blood 2.76E-03 1.37E-01 1.07E+00
Seizure 8A60-8A6Z Whole blood 4.36E-01 -4.41E-02 -3.12E-01
Sensitive skin EK0Z Skin 2.02E-01 9.44E-02 8.97E-01
Sepsis with septic shock 1G41 Whole blood 8.70E-08 1.34E-01 7.71E-01
Shwachman-Diamond syndrome 3A70.0 Bone marrow 3.49E-01 -2.10E-02 -1.01E-01
Sickle cell disease 3A51.0-3A51.3 Peripheral blood 1.39E-01 1.57E-01 8.93E-01
Simpson golabi behmel syndrome LD2C Adipose tissue 8.75E-01 -8.60E-04 -5.79E-03
Sjogren's syndrome 4A43.2 Salivary gland tissue 4.81E-01 -2.12E-02 -1.01E-01
Skin cancer 2C30-2C3Z Skin 2.53E-02 -1.00E-02 -3.52E-02
Thrombocythemia 3B63 Whole blood 3.40E-01 -2.61E-02 -3.07E-01
Thrombocytopenia 3B64 Whole blood 6.04E-01 -1.66E-01 -3.93E-01
Thyroid cancer 2D10 Thyroid 4.04E-01 -2.77E-02 -1.38E-01
Tibial muscular dystrophy 8C75 Muscle tissue 1.72E-03 -1.74E-01 -8.86E-01
Tuberous sclerosis complex LD2D.2 Perituberal tissue 3.51E-01 -3.82E-02 -3.35E-01
Type 2 diabetes 5A11 Liver tissue 9.44E-01 7.21E-03 7.84E-02
Ureter cancer 2C92 Urothelium 6.44E-02 -9.69E-02 -8.84E-01
Uterine cancer 2C78 Endometrium tissue 8.60E-03 -4.92E-02 -2.70E-01
Vitiligo ED63.0 Skin 3.46E-02 2.02E-01 1.00E+00
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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 Protein-tyrosine phosphatase 1B (PTP1B) DTT Info
DME DTT Type Clinical trial
4 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
IONIS-PTP1BRX DMGTJUP Type-2 diabetes 5A11 Phase 2 [1]
TTP-814 DMH9RGV Diabetic complication 5A2Y Phase 1/2 [2]
KQ-791 DMK0BTN Type-2 diabetes 5A11 Phase 1 [1]
Trodusquemine DMQ7UN6 Breast cancer 2C60-2C65 Phase 1 [3]
1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
JTT-551 DM48HVI Type-2 diabetes 5A11 Terminated [4]

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 Protein tyrosine phosphatase 1B (PTP-1B; PTPN1). SciBX 5(7); doi:10.1038/scibx.2012.176. Feb. 16 2012
3 Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-23.
4 Pharmacological effects of JTT-551, a novel protein tyrosine phosphatase 1B inhibitor, in diet-induced obesity mice. J Diabetes Res. 2014;2014:680348.
5 Residues distant from the active site influence protein-tyrosine phosphatase 1B inhibitor binding. J Biol Chem. 2006 Feb 24;281(8):5258-66.