myeloperoxidase

Target id: 2789

Nomenclature: myeloperoxidase

Family: 1.-.-.- Oxidoreductases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     myeloperoxidase has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 745 17q21.3-q23 MPO myeloperoxidase
Mouse - 718 11 C Mpo myeloperoxidase
Rat - 458 10q26 Mpo myeloperoxidase
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 28 [PMID: 28671460] Hs Inhibition 7.4 pIC50 2
pIC50 7.4 (IC50 4.4x10-8 M) [2]
AZD5904 Hs Inhibition 6.7 pIC50 3
pIC50 6.7 (IC50 2x10-7 M) [3]
Description: Inhibition of the chlorination activity of MPO
Immunopharmacology Comments
The peroxidase enzymatic activity of MPO generates hypohalous acids that constitute the major component responsible for neutrophil antimicrobial activity., and as such MPO participates in the innate immune defense mechanism. Since the discovery that MPO-derived oxidants contribute towards the propagation of inflammatory diseases, the pharma industry has been on the hunt for drug-like inhibitors of pathological MPO activity [1].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process ID:  2
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  neutrophil degranulation (GO:0043312) TAS
References: 
Immuno Process:  Cellular signalling
Immuno Process ID:  11
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  neutrophil degranulation (GO:0043312) TAS
References: 
Clinically-Relevant Mutations and Pathophysiology
Disease:  Alzheimer disease
Synonyms: Alzheimer's disease [Disease Ontology: DOID:10652]
Disease Ontology: DOID:10652
OMIM: 104300
Disease:  Myeloperoxidase deficiency; MPOD
OMIM: 254600
Orphanet: ORPHA2587
General Comments
Myeloperoxidase (MPO) is a heme enzyme that participates in the formation of microbicidal reactive oxidants. It is most abundantly expressed in neutrophil granulocytes.

References

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1. Malle E, Furtmüller PG, Sattler W, Obinger C. (2007) Myeloperoxidase: a target for new drug development?. Br. J. Pharmacol.152 (6): 838-54. [PMID:17592500]

2. Soubhye J, Chikh Alard I, Aldib I, Prévost M, Gelbcke M, De Carvalho A, Furtmüller PG, Obinger C, Flemmig J, Tadrent S et al.. (2017) Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. J. Med. Chem.60 (15): 6563-6586. [PMID:28671460]

3. Tidén AK, Sjögren T, Svensson M, Bernlind A, Senthilmohan R, Auchère F, Norman H, Markgren PO, Gustavsson S, Schmidt S et al.. (2011) 2-thioxanthines are mechanism-based inactivators of myeloperoxidase that block oxidative stress during inflammation. J. Biol. Chem.286 (43): 37578-89. [PMID:21880720]

How to cite this page

1.-.-.- Oxidoreductases: myeloperoxidase. Last modified on 02/10/2017. Accessed on 12/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2789.