Page last updated: 2024-08-07 23:00:48
Prostaglandin E synthase
A prostaglandin E synthase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O14684]
Synonyms
EC 5.3.99.3;
Glutathione peroxidase PTGES;
1.11.1.-;
Glutathione transferase PTGES;
2.5.1.18;
Microsomal glutathione S-transferase 1-like 1;
MGST1-L1;
Microsomal prostaglandin E synthase 1;
MPGES-1;
p53-induced gene 12
Research
Bioassay Publications (42)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (9.52) | 29.6817 |
| 2010's | 37 (88.10) | 24.3611 |
| 2020's | 1 (2.38) | 2.80 |
Compounds (34)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ml-3000 | Homo sapiens (human) | EC50 | 0.1000 | 1 | 1 |
Identification of novel mPGES-1 inhibitors through screening of a chemical library.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1.European journal of medicinal chemistry, , Volume: 48, 2012
Novel human mPGES-1 inhibitors identified through structure-based virtual screening.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
Inhibition of the enzymes in the leukotriene and prostaglandin pathways in inflammation by 3-aryl isocoumarins.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.European journal of medicinal chemistry, , Jun-10, Volume: 153, 2018
Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1.Journal of natural products, , Jun-27, Volume: 77, Issue:6, 2014
Effect of phospholipid-based formulations of Boswellia serrata extract on the solubility, permeability, and absorption of the individual boswellic acid constituents present.Journal of natural products, , Oct-26, Volume: 75, Issue:10, 2012
Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.European journal of medicinal chemistry, , Jun-10, Volume: 153, 2018
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.Journal of natural products, , Dec-24, Volume: 78, Issue:12, 2015
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1.Chemical biology & drug design, , Volume: 83, Issue:6, 2014
Discovery of N-amido-phenylsulfonamide derivatives as novel microsomal prostaglandin EBioorganic & medicinal chemistry letters, , 06-01, Volume: 41, 2021
Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.European journal of medicinal chemistry, , Jun-10, Volume: 153, 2018
Evaluation of Dual 5-Lipoxygenase/Microsomal Prostaglandin E2 Synthase-1 Inhibitory Effect of Natural and Synthetic Acronychia-Type Isoprenylated Acetophenones.Journal of natural products, , 03-24, Volume: 80, Issue:3, 2017
[no title available]Journal of natural products, , 03-24, Volume: 80, Issue:3, 2017
Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 26, Issue:1, 2016
2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors.Bioorganic & medicinal chemistry, , Feb-15, Volume: 24, Issue:4, 2016
Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Effects of novel diarylpentanoid analogues of curcumin on secretory phospholipase A2 , cyclooxygenases, lipo-oxygenase, and microsomal prostaglandin E synthase-1.Chemical biology & drug design, , Volume: 83, Issue:6, 2014
Tetra- and pentacyclic triterpene acids from the ancient anti-inflammatory remedy frankincense as inhibitors of microsomal prostaglandin E(2) synthase-1.Journal of natural products, , Jun-27, Volume: 77, Issue:6, 2014
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Fragment-based discovery of novel and selective mPGES-1 inhibitors Part 1: identification of sulfonamido-1,2,3-triazole-4,5-dicarboxylic acid.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Novel benzoxazole inhibitors of mPGES-1.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Identification of novel mPGES-1 inhibitors through screening of a chemical library.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 22, Issue:24, 2012
Pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1.European journal of medicinal chemistry, , Volume: 48, 2012
Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1.Bioorganic & medicinal chemistry, , Jun-01, Volume: 19, Issue:11, 2011
Discovery and biological evaluation of a novel class of dual microsomal prostaglandin E2 synthase-1/5-lipoxygenase inhibitors based on 2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Lignan derivatives from Krameria lappacea roots inhibit acute inflammation in vivo and pro-inflammatory mediators in vitro.Journal of natural products, , Aug-26, Volume: 74, Issue:8, 2011
Novel human mPGES-1 inhibitors identified through structure-based virtual screening.Bioorganic & medicinal chemistry, , Oct-15, Volume: 19, Issue:20, 2011
A novel class of dual mPGES-1/5-LO inhibitors based on the α-naphthyl pirinixic acid scaffold.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E(2) synthase-1.Bioorganic & medicinal chemistry, , Dec-01, Volume: 17, Issue:23, 2009
Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).Journal of medicinal chemistry, , Aug-13, Volume: 52, Issue:15, 2009
Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Discovery of furan and dihydrofuran-fused tricyclic benzo[d]imidazole derivatives as potent and orally efficacious microsomal prostaglandin E synthase-1 (mPGES-1) inhibitors: Part-1.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 27, Issue:23, 2017
Tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives as microsomal prostaglandin EBioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
[no title available]Bioorganic & medicinal chemistry letters, , 12-15, Volume: 26, Issue:24, 2016
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
Benzo[d]isothiazole 1,1-dioxide derivatives as dual functional inhibitors of 5-lipoxygenase and microsomal prostaglandin E(2) synthase-1.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Discovery of highly potent microsomal prostaglandin e2 synthase 1 inhibitors using the active conformation structural model and virtual screen.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Novel benzoxazole inhibitors of mPGES-1.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E₂ synthase-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 22, Issue:1, 2012
Trisubstituted ureas as potent and selective mPGES-1 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 19, Issue:20, 2009
Plant-derived mPGES-1 inhibitors or suppressors: A new emerging trend in the search for small molecules to combat inflammation.European journal of medicinal chemistry, , Jun-10, Volume: 153, 2018
Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| glutathione transferase activity | molecular function | Catalysis of the reaction: R-X + glutathione = H-X + R-S-glutathione. R may be an aliphatic, aromatic or heterocyclic group; X may be a sulfate, nitrile or halide group. [EC:2.5.1.18] |
| glutathione peroxidase activity | molecular function | Catalysis of the reaction: 2 glutathione + hydrogen peroxide = oxidized glutathione + 2 H2O. [EC:1.11.1.9, PMID:36771108] |
| prostaglandin-D synthase activity | molecular function | Catalysis of the reaction: prostaglandin H(2) = prostaglandin D(2). [EC:5.3.99.2, RHEA:10600] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| glutathione binding | molecular function | Binding to glutathione; a tripeptide composed of the three amino acids cysteine, glutamic acid and glycine. [GOC:bf, ISBN:0198506732] |
| prostaglandin-E synthase activity | molecular function | Catalysis of the reaction: prostaglandin H(2) = prostaglandin E(2). [EC:5.3.99.3, RHEA:12893] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nuclear envelope lumen | cellular component | The region between the two lipid bilayers of the nuclear envelope; 20-40 nm wide. [GOC:ai] |
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Involved In
This protein is involved in 10 target(s):
| Target | Category | Definition |
|---|
| prostaglandin biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of prostaglandins, any of a group of biologically active metabolites which contain a cyclopentane ring. [GOC:ai] |
| prostaglandin metabolic process | biological process | The chemical reactions and pathways involving prostaglandins, any of a group of biologically active metabolites which contain a cyclopentane ring due to the formation of a bond between two carbons of a fatty acid. They have a wide range of biological activities. [ISBN:0198506732] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| cell population proliferation | biological process | The multiplication or reproduction of cells, resulting in the expansion of a cell population. [GOC:mah, GOC:mb] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| sensory perception of pain | biological process | The series of events required for an organism to receive a painful stimulus, convert it to a molecular signal, and recognize and characterize the signal. Pain is medically defined as the physical sensation of discomfort or distress caused by injury or illness, so can hence be described as a harmful stimulus which signals current (or impending) tissue damage. Pain may come from extremes of temperature, mechanical damage, electricity or from noxious chemical substances. This is a neurological process. [GOC:curators] |
| regulation of fever generation | biological process | Any process that modulates the rate or extent of fever generation. [GOC:add, GOC:dph, GOC:tb] |
| positive regulation of prostaglandin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of a prostaglandin from a cell. [GOC:mah] |
| regulation of inflammatory response | biological process | Any process that modulates the frequency, rate or extent of the inflammatory response, the immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. [GOC:ai] |
| cellular oxidant detoxification | biological process | Any process carried out at the cellular level that reduces or removes the toxicity superoxide radicals or hydrogen peroxide. [GOC:dos, GOC:vw] |