Proteins > Arachidonate 5-lipoxygenase-activating protein
Page last updated: 2024-08-07 13:05:08
Arachidonate 5-lipoxygenase-activating protein
An arachidonate 5-lipoxygenase-activating protein that is encoded in the genome of human. [PRO:DNx, UniProtKB:P20292]
Synonyms
FLAP;
MK-886-binding protein
Research
Bioassay Publications (19)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 3 (15.79) | 18.2507 |
| 2000's | 4 (21.05) | 29.6817 |
| 2010's | 12 (63.16) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (11)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Recent advances for FLAP inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 25, Issue:13, 2015
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 9, Issue:16, 1999
Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Recent development of lipoxygenase inhibitors as anti-inflammatory agents.MedChemComm, , Feb-01, Volume: 9, Issue:2, 2018
Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions.Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Novel benzoxazole inhibitors of mPGES-1.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).Bioorganic & medicinal chemistry, , Jun-15, Volume: 20, Issue:12, 2012
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibJournal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 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
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
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
Enables
This protein enables 10 target(s):
| Target | Category | Definition |
|---|
| arachidonate 5-lipoxygenase activity | molecular function | Catalysis of the reaction: arachidonate + O2 = (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxycosa-6,8,11,14-tetraenoate. [EC:1.13.11.34, RHEA:32307] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| enzyme activator activity | molecular function | Binds to and increases the activity of an enzyme. [GOC:dph, GOC:mah, GOC:tb] |
| enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein-containing complex binding | molecular function | Binding to a macromolecular complex. [GOC:jl] |
| arachidonic acid binding | molecular function | Binding to arachidonic acid, a straight chain fatty acid with 20 carbon atoms and four double bonds per molecule. Arachidonic acid is the all-Z-(5,8,11,14)-isomer. [GOC:ai] |
| 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] |
| leukotriene-C4 synthase activity | molecular function | Catalysis of the reaction: leukotriene C(4) = glutathione + leukotriene A(4). [EC:4.4.1.20, RHEA:17617] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| 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] |
| nuclear membrane | cellular component | Either of the lipid bilayers that surround the nucleus and form the nuclear envelope; excludes the intermembrane space. [GOC:mah, GOC:pz] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| leukotriene production involved in inflammatory response | biological process | The synthesis or release of any leukotriene following a stimulus as part of an inflammatory response, resulting in an increase in its intracellular or extracellular levels. [GOC:add, ISBN:0781735149] |
| positive regulation of acute inflammatory response | biological process | Any process that activates or increases the frequency, rate, or extent of an acute inflammatory response. [GOC:add] |
| leukotriene biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of leukotriene, a pharmacologically active substance derived from a polyunsaturated fatty acid, such as arachidonic acid. [GOC:go_curators] |
| lipoxygenase pathway | biological process | The chemical reactions and pathways by which an unsaturated fatty acid (such as arachidonic acid or linolenic acid) is converted to other compounds, and in which the first step is hydroperoxide formation catalyzed by lipoxygenase. [GOC:mah, PMID:17163881] |
| protein homotrimerization | biological process | The formation of a protein homotrimer, a macromolecular structure consisting of three noncovalently associated identical subunits. [GOC:hjd] |
| cellular response to calcium ion | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a calcium ion stimulus. [GOC:mah] |
| 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] |