Proteins > Platelet-activating factor acetylhydrolase
Page last updated: 2024-08-07 17:04:20
Platelet-activating factor acetylhydrolase
A platelet-activating factor acetylhydrolase that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q13093]
Synonyms
PAF acetylhydrolase;
EC 3.1.1.47;
1-alkyl-2-acetylglycerophosphocholine esterase;
2-acetyl-1-alkylglycerophosphocholine esterase;
Group-VIIA phospholipase A2;
gVIIA-PLA2;
LDL-associated phospholipase A2;
LDL-PLA(2);
PAF 2-
Research
Bioassay Publications (21)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (23.81) | 18.2507 |
| 2000's | 5 (23.81) | 29.6817 |
| 2010's | 11 (52.38) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (18)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ly 171883 | Homo sapiens (human) | IC50 | 18.9000 | 1 | 2 |
| raloxifene | Homo sapiens (human) | IC50 | 0.0003 | 2 | 2 |
| 1,6-bis(cyclohexyloximinocarbonyl)hexane | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| vorinostat | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| 5,5-dimethylhydantoin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| benzenesulfonamide | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| wy 48252 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 2 |
| 4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
| spiroglumide | Homo sapiens (human) | IC50 | 1.2230 | 1 | 1 |
| tamoxifen | Homo sapiens (human) | IC50 | 0.9040 | 1 | 1 |
| orlistat | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
| arachidonyltrifluoromethane | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| manoalide | Homo sapiens (human) | IC50 | 3.9000 | 1 | 1 |
| darapladib | Homo sapiens (human) | IC50 | 0.0003 | 12 | 13 |
| darapladib | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| sb-435495 | Homo sapiens (human) | IC50 | 0.0000 | 2 | 3 |
| sb-435495 | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | Homo sapiens (human) | IC50 | 0.0730 | 1 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| benzenesulfonamide | Homo sapiens (human) | Kd | 3,400.0000 | 1 | 1 |
| darapladib | Homo sapiens (human) | Kd | 0.0497 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| vitamin k 3 | Homo sapiens (human) | Km | 72.0000 | 1 | 5 |
| plumbagin | Homo sapiens (human) | Km | 74.0000 | 1 | 5 |
Synthesis and biological activity of trans-2,3-dihydroraloxifene.Bioorganic & medicinal chemistry letters, , Apr-19, Volume: 9, Issue:8, 1999
Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene.Journal of medicinal chemistry, , Jan-17, Volume: 40, Issue:2, 1997
Regioselectivity of thiouracil alkylation: Application to optimization of Darapladib synthesis.Bioorganic & medicinal chemistry letters, , 02-15, Volume: 28, Issue:4, 2018
Investigation of a Bicyclo[1.1.1]pentane as a Phenyl Replacement within an LpPLAACS medicinal chemistry letters, , Jan-12, Volume: 8, Issue:1, 2017
Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2.Journal of medicinal chemistry, , 12-28, Volume: 60, Issue:24, 2017
Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening.Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular Edema.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Fragment-Based Approach to the Development of an Orally Bioavailable Lactam Inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLAJournal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Triazole derivatives: a series of Darapladib analogues as orally active Lp-PLA2 inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.Bioorganic & medicinal chemistry letters, , Sep-16, Volume: 12, Issue:18, 2002
Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kJournal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| 1-alkyl-2-acetylglycerophosphocholine esterase activity | molecular function | Catalysis of the reaction: 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine + H2O = 1-alkyl-sn-glycero-3-phosphocholine + acetate. [EC:3.1.1.47] |
| phospholipid binding | molecular function | Binding to a phospholipid, a class of lipids containing phosphoric acid as a mono- or diester. [ISBN:0198506732] |
| hydrolase activity, acting on ester bonds | molecular function | Catalysis of the hydrolysis of any ester bond. [GOC:jl] |
| calcium-independent phospholipase A2 activity | molecular function | Catalysis of the reaction: phosphatidylcholine + H2O = 1-acylglycerophosphocholine + a carboxylate. This reaction does not require Ca2+. [EC:3.1.1.4] |
Located In
This protein is located in 1 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] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| low-density lipoprotein particle | cellular component | A lipoprotein particle, rich in cholesterol esters and low in triglycerides that is typically composed of APOB100 and APOE and has a density of 1.02-1.06 g/ml and a diameter of between 20-25 nm. LDL particles are formed from VLDL particles (via IDL) by the loss of triglyceride and gain of cholesterol ester. They transport endogenous cholesterol (and to some extent triglycerides) from peripheral tissues back to the liver. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:rl] |
| high-density lipoprotein particle | cellular component | A lipoprotein particle with a high density (typically 1.063-1.21 g/ml) and a diameter of 5-10 nm that contains APOAs and may contain APOCs and APOE; found in blood and carries lipids from body tissues to the liver as part of the reverse cholesterol transport process. [GOC:BHF, GOC:expert_pt, GOC:mah, GOC:pde, GOC:rl] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| peptide hormone processing | biological process | The generation of a mature peptide hormone by posttranslational processing of a prohormone. [GOC:mah] |
| 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] |
| lipid oxidation | biological process | The removal of one or more electrons from a lipid, with or without the concomitant removal of a proton or protons, by reaction with an electron-accepting substance, by addition of oxygen or by removal of hydrogen. [GOC:BHF, GOC:mah] |
| plasma lipoprotein particle oxidation | biological process | The modification of a lipid or protein within a plasma lipoprotein particle by oxidation of the lipid or one or more amino acids. [GOC:BHF, GOC:mah] |
| phosphatidylcholine catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of phosphatidylcholines, any of a class of glycerophospholipids in which the phosphatidyl group is esterified to the hydroxyl group of choline. [GOC:jp] |
| platelet activating factor metabolic process | biological process | The chemical reactions and pathways involving platelet activating factor, 1-O-alkyl-2-acetyl-sn-glycerol 3-phosphocholine, where alkyl = hexadecyl or octadecyl. Platelet activating factor is an inflammatory mediator released from a variety of cells in response to various stimuli. [ISBN:0198547684] |
| positive regulation of inflammatory response | biological process | Any process that activates or increases the frequency, rate or extent of the inflammatory response. [GOC:ai] |
| platelet activating factor catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of platelet activating factor, 2-O-acetyl-1-O-octadecyl-sn-glycero-3-phosphocholine. [PMID:16371369] |
| positive regulation of monocyte chemotaxis | biological process | Any process that increases the frequency, rate, or extent of monocyte chemotaxis. [GOC:dph, GOC:tb] |