Page last updated: 2024-08-07 15:39:40
Myeloperoxidase
A myeloperoxidase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P05164]
Synonyms
MPO;
EC 1.11.2.2
Research
Bioassay Publications (13)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (7.69) | 29.6817 |
| 2010's | 10 (76.92) | 24.3611 |
| 2020's | 2 (15.38) | 2.80 |
Compounds (31)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| melatonin | Homo sapiens (human) | IC50 | 3.0000 | 1 | 1 |
| 4-hydroxybenzoic acid hydrazide | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| aspirin | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| dapsone | Homo sapiens (human) | IC50 | 0.4200 | 1 | 1 |
| hydralazine | Homo sapiens (human) | IC50 | 1.2650 | 4 | 4 |
| isoniazid | Homo sapiens (human) | IC50 | 4.8500 | 2 | 2 |
| mefenamic acid | Homo sapiens (human) | IC50 | 1.5950 | 2 | 2 |
| metoclopramide | Homo sapiens (human) | IC50 | 2.6750 | 2 | 2 |
| nimesulide | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
| o(6)-benzylguanine | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| tryptophan | Homo sapiens (human) | IC50 | 2.2500 | 1 | 1 |
| 4-aminobenzhydrazide | Homo sapiens (human) | IC50 | 0.3000 | 2 | 2 |
| paroxetine | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
| salicylhydroxamic acid | Homo sapiens (human) | IC50 | 14.0000 | 2 | 2 |
| 5-fluorotryptamine | Homo sapiens (human) | IC50 | 0.8650 | 2 | 2 |
| sb 203580 | Homo sapiens (human) | Ki | 0.0900 | 1 | 1 |
| 2-guanidine-4-methylquinazoline | Homo sapiens (human) | IC50 | 0.9000 | 1 | 1 |
| propylthiouracil | Homo sapiens (human) | IC50 | 2.8100 | 1 | 1 |
| levosulpiride | Homo sapiens (human) | IC50 | 7.6800 | 1 | 1 |
| 2-(1-piperidinylmethyl)phenol | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 2-[[3-[(2-hydroxyphenyl)methyl]-1,3-diazinan-1-yl]methyl]phenol | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 1.6975 | 4 | 4 |
| apigenin | Homo sapiens (human) | IC50 | 3.8000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 2.2400 | 1 | 1 |
| 4',7-dihydroxyflavone | Homo sapiens (human) | IC50 | 5.7900 | 1 | 1 |
| (3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone | Homo sapiens (human) | Ki | 0.0019 | 1 | 1 |
| nifuroxazide | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| N-(3-cyanophenyl)-2'-methyl-5'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl-4-carboxamide | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| azd3241 | Homo sapiens (human) | IC50 | 0.6300 | 2 | 2 |
| pf-06282999 | Homo sapiens (human) | IC50 | 17.8435 | 2 | 2 |
| pf-06282999 | Homo sapiens (human) | Ki | 0.3162 | 1 | 1 |
| phthivazide | Homo sapiens (human) | IC50 | 0.4600 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| salicylhydroxamic acid | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
From Dynamic Combinatorial Chemistry to ACS medicinal chemistry letters, , Feb-09, Volume: 8, Issue:2, 2017
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
The development of myeloperoxidase inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 29, Issue:1, 2019
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Potent reversible inhibition of myeloperoxidase by aromatic hydroxamates.The Journal of biological chemistry, , Dec-20, Volume: 288, Issue:51, 2013
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Structure-based design, synthesis, and pharmacological evaluation of 3-(aminoalkyl)-5-fluoroindoles as myeloperoxidase inhibitors.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
The development of myeloperoxidase inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 29, Issue:1, 2019
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).Bioorganic & medicinal chemistry, , 06-15, Volume: 28, Issue:12, 2020
The development of myeloperoxidase inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 29, Issue:1, 2019
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction.Journal of medicinal chemistry, , 09-08, Volume: 65, Issue:17, 2022
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
| peroxidase activity | molecular function | Catalysis of the reaction: a donor + a peroxide = an oxidized donor + 2 H2O. [GOC:curators] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| heparin binding | molecular function | Binding to heparin, a member of a group of glycosaminoglycans found mainly as an intracellular component of mast cells and which consist predominantly of alternating alpha-(1->4)-linked D-galactose and N-acetyl-D-glucosamine-6-sulfate residues. [GOC:jl, ISBN:0198506732] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| lysosome | cellular component | A small lytic vacuole that has cell cycle-independent morphology found in most animal cells and that contains a variety of hydrolases, most of which have their maximal activities in the pH range 5-6. The contained enzymes display latency if properly isolated. About 40 different lysosomal hydrolases are known and lysosomes have a great variety of morphologies and functions. [GOC:mah, ISBN:0198506732] |
| secretory granule | cellular component | A small subcellular vesicle, surrounded by a membrane, that is formed from the Golgi apparatus and contains a highly concentrated protein destined for secretion. Secretory granules move towards the periphery of the cell and upon stimulation, their membranes fuse with the cell membrane, and their protein load is exteriorized. Processing of the contained protein may take place in secretory granules. [GOC:mah, ISBN:0198506732] |
| azurophil granule lumen | cellular component | The volume enclosed by the membrane of an azurophil granule, a primary lysosomal granule found in neutrophil granulocytes that contains a wide range of hydrolytic enzymes and is released into the extracellular fluid. [GOC:bf, PMID:17152095] |
| azurophil granule | cellular component | Primary lysosomal granule readily stainable with a Romanowsky stain. [GOC:jl, PMID:17152095, PMID:28717070, PMID:5914694, WIKIPEDIA:Azurophilic_granule] |
| intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| phagocytic vesicle lumen | cellular component | The volume enclosed by the membrane of a phagocytic vesicle. [GOC:rs] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 15 target(s):
| Target | Category | Definition |
|---|
| response to yeast | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a yeast species. [PMID:14707091] |
| hypochlorous acid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of hypochlorous acid. [GOC:add, PMID:10085024, PMID:176150] |
| respiratory burst involved in defense response | biological process | A phase of elevated metabolic activity, during which oxygen consumption increases made as part of a defense response ; this leads to the production, by an NADH dependent system, of hydrogen peroxide (H2O2), superoxide anions and hydroxyl radicals. [GOC:add, ISBN:0781735149, PMID:12789499] |
| defense response | biological process | Reactions, triggered in response to the presence of a foreign body or the occurrence of an injury, which result in restriction of damage to the organism attacked or prevention/recovery from the infection caused by the attack. [GOC:go_curators] |
| response to oxidative stress | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, e.g. superoxide anions, hydrogen peroxide (H2O2), and hydroxyl radicals. [GOC:jl, PMID:12115731] |
| response to mechanical stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mechanical stimulus. [GOC:hb] |
| removal of superoxide radicals | biological process | Any process, acting at the cellular level, involved in removing superoxide radicals (O2-) from a cell or organism, e.g. by conversion to dioxygen (O2) and hydrogen peroxide (H2O2). [GOC:jl] |
| response to food | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a food stimulus; food is anything which, when taken into the body, serves to nourish or build up the tissues or to supply body heat. [GOC:add, ISBN:0721601464] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| low-density lipoprotein particle remodeling | biological process | The acquisition, loss or modification of a protein or lipid within a low-density lipoprotein particle, including the hydrolysis of triglyceride by hepatic lipase, with the subsequent loss of free fatty acid, and the transfer of cholesterol esters from LDL to a triglyceride-rich lipoprotein particle by cholesteryl ester transfer protein (CETP), with the simultaneous transfer of triglyceride to LDL. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| hydrogen peroxide catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of hydrogen peroxide (H2O2). [GOC:jl] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| defense response to fungus | biological process | Reactions triggered in response to the presence of a fungus that act to protect the cell or organism. [GOC:ai] |
| response to gold nanoparticle | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a gold nanoparticle stimulus. [PMID:23150627] |
| defense response to bacterium | biological process | Reactions triggered in response to the presence of a bacterium that act to protect the cell or organism. [GOC:jl] |