Target Information
| Target General Information | Top | |||||
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| Target ID |
T23471
(Former ID: TTDC00199)
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| Target Name |
Myeloperoxidase (MPO)
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| Synonyms |
MPO
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| Gene Name |
MPO
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Postoperative inflammation [ICD-11: 1A00-CA43] | |||||
| Function |
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acidin physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity.
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| BioChemical Class |
Peroxidases
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| UniProt ID | ||||||
| EC Number |
EC 1.11.2.2
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| Sequence |
MGVPFFSSLRCMVDLGPCWAGGLTAEMKLLLALAGLLAILATPQPSEGAAPAVLGEVDTS
LVLSSMEEAKQLVDKAYKERRESIKQRLRSGSASPMELLSYFKQPVAATRTAVRAADYLH VALDLLERKLRSLWRRPFNVTDVLTPAQLNVLSKSSGCAYQDVGVTCPEQDKYRTITGMC NNRRSPTLGASNRAFVRWLPAEYEDGFSLPYGWTPGVKRNGFPVALARAVSNEIVRFPTD QLTPDQERSLMFMQWGQLLDHDLDFTPEPAARASFVTGVNCETSCVQQPPCFPLKIPPND PRIKNQADCIPFFRSCPACPGSNITIRNQINALTSFVDASMVYGSEEPLARNLRNMSNQL GLLAVNQRFQDNGRALLPFDNLHDDPCLLTNRSARIPCFLAGDTRSSEMPELTSMHTLLL REHNRLATELKSLNPRWDGERLYQEARKIVGAMVQIITYRDYLPLVLGPTAMRKYLPTYR SYNDSVDPRIANVFTNAFRYGHTLIQPFMFRLDNRYQPMEPNPRVPLSRVFFASWRVVLE GGIDPILRGLMATPAKLNRQNQIAVDEIRERLFEQVMRIGLDLPALNMQRSRDHGLPGYN AWRRFCGLPQPETVGQLGTVLRNLKLARKLMEQYGTPNNIDIWMGGVSEPLKRKGRVGPL LACIIGTQFRKLRDGDRFWWENEGVFSMQQRQALAQISLPRIICDNTGITTVSKNNIFMS NSYPRDFVNCSTLPALNLASWREAS Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| ADReCS ID | BADD_A00127 ; BADD_A01943 ; BADD_A02053 ; BADD_A02603 ; BADD_A03271 ; BADD_A03824 ; BADD_A04537 ; BADD_A04561 ; BADD_A06206 ; BADD_A07267 | |||||
| HIT2.0 ID | T30VNV | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | E-101 | Drug Info | Phase 3 | Infectious disease | [2] | |
| 2 | AZD-3241 | Drug Info | Phase 2 | Parkinson disease | [3] | |
| 3 | AZD4831 | Drug Info | Phase 1 | Heart failure | [4] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | AZD5904 | Drug Info | Discontinued in Phase 1 | Multiple sclerosis | [5], [6] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | E-101 | Drug Info | [1] | |||
| 2 | AZD4831 | Drug Info | [4] | |||
| Inhibitor | [+] 4 Inhibitor drugs | + | ||||
| 1 | AZD-3241 | Drug Info | [7] | |||
| 2 | AZD5904 | Drug Info | [8] | |||
| 3 | 4-aminobenzoic acid hydrazide | Drug Info | [9] | |||
| 4 | INV-311 | Drug Info | [10] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Phagosome | |||||
| 2 | Transcriptional misregulation in cancer | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | C-MYB transcription factor network | |||||
| 2 | IL23-mediated signaling events | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Folate Metabolism | |||||
| 2 | Vitamin B12 Metabolism | |||||
| 3 | Selenium Micronutrient Network | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | In vitro antibacterial activity of E-101 Solution, a novel myeloperoxidase-mediated antimicrobial, against Gram-positive and Gram-negative pathogens. J Antimicrob Chemother. 2011 Feb;66(2):335-42. | |||||
| REF 2 | ClinicalTrials.gov (NCT01297959) Efficacy and Safety of E-101 Solution for Preventing Surgical Site Infections After Colorectal Surgery. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT02388295) AZD3241 PET MSA Trial, Phase 2, Randomized,12 Week Safety and Tolerability Trial With PET in MSA Patients. U.S. National Institutes of Health. | |||||
| REF 4 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 5 | 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: 7728). | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024670) | |||||
| REF 7 | Effect of the myeloperoxidase inhibitor AZD3241 on microglia: a PET study in Parkinson's disease. Brain. 2015 Sep;138(Pt 9):2687-700. | |||||
| REF 8 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
| REF 9 | Myeloperoxidase expression as a potential determinant of parthenolide-induced apoptosis in leukemia bulk and leukemia stem cells. J Pharmacol Exp Ther. 2010 Nov;335(2):389-400. | |||||
| REF 10 | 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. (Target id: 2789). | |||||
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