5 lipoxygenase activating protein inhibitors. Medical search. Frequent questions

AM-679 is a drug which acts as a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). (wikipedia.org)
Abnormal expression of 5-Lipoxygenase Activating Protein (FLAP) has been detected in many tumor cells. (biomedcentral.com)
We demonstrated that miR-146a expression is overexpressed, while FLAP protein and mRNA are suppressed in hepatocellular carcinoma tissues and HepG2 cells compared to para-carcinoma tissues and HL-7702 cells. (biomedcentral.com)
The metabolic pathway of arachidonic acid (AA) has two main branches: 1) AA is converted by COX-1 and COX-2 into prostaglandins (PG) and thromboxane (TX), and 2) the actions of 5-lipoxygenase (5-LO) and 5-Lipoxygenase Activating Protein (FLAP) create leukotrienes (LT) in the other arm of the pathway [ 16 ]. (biomedcentral.com)
MK-886 is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). (targetmol.jp)
Upon stimulation of the cell, 5-LO translocates to the nuclear membrane where it is found in association with 5-LO activating protein (FLAP) and with the 85 kDa cPLA 2 . (sigmaaldrich.com)
It translocates to the nuclear membrane upon stimulation, where it co-localizes with 5-LOX activating protein (FLAP) and cytosolic phospholipase A 2 (cPLA 2 ) [ 5 ]. (biomedcentral.com)
Emerging data implicate both 5-LOX and FLAP in the disease process of cerebral ischemia [ 6 ]. (biomedcentral.com)

One of the primary causes of ARF is ischemia/reperfusion (I/R). Inflammatory process and oxidative stress are thought to be the major mechanisms causing I/R. MK-886 is a potent inhibitor of leukotrienes biosynthesis which may have anti-inflammatory and antioxidant effects through inhibition of polymorphonuclear leukocytes (PMNs) infiltration into renal tissues. (biomedcentral.com)

This protein is involved in the production of cysteinyl leukotrienes which are involved in inflammation, and AM-679 has anti-inflammatory effects in animal studies. (wikipedia.org)
Cysteinyl leukotrienes (Cys-LTs) are potent inflammatory lipid mediators derived from the 5-lypoxygenase (5-LO) pathway of arachidonic acid (AA) metabolism [ 1 ], initially identified to have important effects on pathogenetic aspects of allergic rhinitis and bronchial asthma and approved in the late 1990s for the relief of perennial and seasonal allergic rhinitis symptoms, and the treatment of mild persistent bronchial asthma [ 2 - 5 ]. (hindawi.com)
Upon exposure to an initiating stimulus (an asthma inducer), these inflammatory cells release inflammatory mediators such as histamine, leukotrienes, prostaglandins, cytokines, chemokines, and platelet-activating factor. (respiratory-therapy.com)
previously named ML3000) is a substrate analogue of arachidonic acid which inhibits cyclooxygenase type 1 and 2 (COX1 and COX2) and 5-lipoxygenase (5-LOX), decreasing prostaglandins and leukotrienes production. (j-epilepsy.org)
Leukotrienes derived from 5-lipoxygenase (5-LOX) cause inflammation and are thus involved in the pathobiology of stroke injury. (biomedcentral.com)
Leukotrienes (LTs) are lipid mediators derived from the 5-lipoxygenase pathway of arachidonic acid metabolism. (springer.com)

5-Lipoxygenase, Human, Recombinant, S. fruigiperda 5-Lipoxygenase, Human, Recombinant, S. frugiperda E.C 1.13.11.34, catalyzes the formation of 5(S)-HpETE from arachidonic acid and its subsequent conversion to leukotriene A4. (sigmaaldrich.com)
5-LO catalyzes the formation of 5(S)-HpETE from arachidonic acid and its subsequent conversion to leukotriene A 4 . (sigmaaldrich.com)

To test the neuroprotective efficacy of 5-LOX inhibition in a rat model of focal cerebral IR, ischemic animals were either pre- or post-treated with a potent selective 5-LOX inhibitor, (N- [3-[3-(-fluorophenoxy) phenyl]-1-methyl-2-propenyl]- N -hydroxyurea (BW-B 70C). (biomedcentral.com)
Kaithwas, Gaurav 2019-10-24 00:00:00 Background: This study evaluates the anti-cancer effects of Tadalafil (potent PDE-5 inhibitor) in female albino wistar rats against n-methyl n-nitrosourea induced mammary gland carcinogenesis. (sagepub.com)
Furthermore, LysoPLs are also the precursors of platelet activating factor (PAF), possibly the most potent mediator of inflammatory processes. (drugdiscoverynews.com)

AACOCF 3 , a phospholipase A 2 (PLA 2 ) inhibitor, strongly abrogated chemosensitization upon silencing of S100A11 suggesting that PLA 2 inhibition by S100A11 governs the chemoresistance of NSCLC. (oncotarget.com)

Singh D, Boyce M, Norris V, Kent S, Bentley J. Inhibition of the early asthmatic response to inhaled allergen by the 5-lipoxygenase activating protein inhibitor GSK2190915: a dose-response study. (hmrlondon.com)
The enhancing effect was also evident with endogenous cysLTs produced from immunologically activated mast cells because inhibition of cysLT action by montelukast or cysLT synthesis by MK886, an inhibitor of 5-lipoxygenase-activating protein, reduced the response of Th2 cells to the levels produced by PGD(2) alone. (ox.ac.uk)
It further inhibited cell-cycle progression in the G1 phase by four different mechanisms: rapid downregulation of cyclin D1, induction of Chk2 with simultaneous downregulation of Cdc25A, induction of the Cdk-inhibitor p21 Cip/Waf and inhibition of ribonucleotide reductase activity resulting in reduced dCTP and dTTP levels. (nature.com)
The study demonstrates the neuroprotective potential of 5-LOX inhibition through down-regulation of NF-κB in a rat model of experimental stroke. (biomedcentral.com)

Digalloyl-resveratrol (di-GA) is a synthetic compound aimed to combine the biological effects of the plant polyhydroxy phenols gallic acid and resveratrol, which are both radical scavengers and cyclooxygenase inhibitors exhibiting anticancer activity. (nature.com)
Licofelone is a cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor, which its effectiveness to treat osteoarthritis has been approved. (j-epilepsy.org)
The cell-free media from MWCNT-polarized macrophages induced the migration of neutrophilic cells (differentiated from HL-60), which was blocked by Acebilustat, a specific leukotriene A4 hydrolase inhibitor, or LY239111, an LTB4 receptor antagonist, but not NS-398, a cyclooxygenase 2 inhibitor, revealing LTB4 as a major mediator of neutrophil chemotaxis from MWCNT-polarized macrophages. (cdc.gov)

A novel inhaled phosphodiesterase 4 inhibitor (CHF6001) reduces the allergen challenge response in asthmatic patients. (hmrlondon.com)
Tadalafil is a known phosphodiesterase-5 Distinct metastasis and resistance development by self- (PDE-5) inhibitor, which have anti-cancer effects in vari- renewing nascent cancer cells in response with the ous types of cancer [2]. (sagepub.com)
Moreover, phosphodiesterase 4D (PDE4D) [ 13 ], and 5-lipoxygenase gene activating protein (ALOX5AP) [ 14 ], were shown to be significantly related with ischemic stroke due to progressive changes in the walls of blood vessels resulting in the increased atherosclerosis process. (biomedcentral.com)

For these, reasons both leukotriene synthesis inhibitors and leukotriene receptor antagonists have been suggested for inducing beneficial effects at different stages of the atherosclerosis process and may represent a new therapeutic target in the treatment of atherosclerotic vessel diseases, in particular in acute coronary syndrome. (hindawi.com)
Cholinergic muscarinic receptors are members of the G-protein coupled receptor super-family and are further divided into 5 subtypes, M 1 to M 5 . (justia.com)
In the field of molecular biology, the peroxisome proliferator-activated receptors (PPARs) are a group of nuclear receptor proteins that function as transcription factors regulating the expression of genes. (targetmol.jp)
INT-131, is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment. (targetmol.jp)
Moreover, we investigated the effects of RvD1 on IL-4-induced activation of signal transducer and activators of transcription 6 (STAT6) and peroxisome proliferator-activated receptor gamma (PPARγ). (biomedcentral.com)
CD45 (LCA, leukocyte common antigen) is a receptor-type protein tyrosine phosphatase (PTP) ubiquitously expressed in all nucleated hematopoietic cells, comprising approximately 10% of all surface proteins in lymphocytes. (thermofisher.com)

MNU 47 mg/kg, i.v.) and group IV (Tada- activate protein kinase G and map kinase pathway of lafil 4 mg/kg, p.o. (sagepub.com)

Inflammation which comprises a rapid, short-lived, relatively uniform response to acute injury or antigenic challenge and is characterized by accumulations of fluid, plasma proteins, and granulocytic leukocytes. (gsea-msigdb.org)
TNF Alpha Inhibitors Market Overview 2023-2032 - Market Growth Analysis, Trends And Drivers - TNF alpha inhibitors refer to medications that are used to treat inflammatory diseases such as rheumatoid arthritis (RA), psoriatic arthritis, and juvenile idiopathic arthritis and that help to reduce or eliminate inflammation. (powershow.com)

3, 5-diiodothyropropionic acid (DITPA) have evidences of improving effects on I/R in heart through modulation of cellular signaling in response to ischemic stress. (biomedcentral.com)
Two other structurally different 5-LOX inhibitors were also administered post IR: caffeic acid and 2, 3, 5-trimethyl-6- [12-hydroxy-5, 10-dodecadiynyl]-1, 4-benzoquinone (AA-861). (biomedcentral.com)
MNU was dissolved im- (cAMP) and cyclic guanosine monophosphate (cGMP) mediately before use in glacial acetic acid and water (pH into their intermediate inactive 50 derivatives and 5- 4.5-5). (sagepub.com)
The plant C18 fatty acids, linoleic acid and linolenic acid, can be converted by the enzymes a -dioxygenase, 9- or 13-lipoxygenase, giving rise to a multitude of oxylipins. (gerli.com)

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC5. (targetmol.jp)
Further, the effects of RvD1 and IL-4 on Arg1 and Ym1 were blocked by the application of leflunomide (a STAT6 inhibitor) or GW9662 (a PPARγ antagonist). (biomedcentral.com)

Furthermore, activated miR-146a inhibited cancer migration, invasion, and metastasis by downregulating vascular endothelial growth factor through dual pathways in HCC. (biomedcentral.com)
Also, we suggest that COX/5-LOX activation is possibly required in the initial stage of onset but SE recruits extra excitatory pathways with prolongation. (j-epilepsy.org)
Recently, we have demonstrated that PLA 2 and 5-LOX are involved in lipopolysaccharide (LPS)-induced iNOS gene expression via dependent and independent NF-κB pathways in glial cells [ 11 ]. (biomedcentral.com)
Induction of growth factors [interleukin 6 (IL-6), insulin-like growth factor-1, and vascular endothelial growth factor/platelet-derived growth factor) may indirectly activate the AR and/or its downstream signaling pathways (5, 6, 7) . (aacrjournals.org)
GSE-related anti-cancer activity mostly relies on the induced increase in reactive oxygen species, followed by the orchestrated down- and up-regulation of several key-molecular pathways, including MAPK kinases, PI3K/Akt, NF-kB, cytoskeleton proteins and metalloproteinases. (oatext.com)

The AA, a normal component of cell membrane phospholipids, serve as substrate for prostaglandin endoperoxide (PGH) syntases-1 and -2, also known as cycloxygenase (COX)-1 and -2, lipoxygenase (5-, 12-, or 15) (LO), or cytochrome p450 enzymes [ 18 ]. (hindawi.com)
The 5-, 12- and 15-HETE are the main forms but others have been detected (8-, 9-, 11-, 15-, 17-, 18-, 19- and 20-HETE, the 16- to 20-HETE being formed via cytochrome P450). (gerli.com)

The effect of LTE(4) was inhibited by montelukast but not by the P2Y(12) antagonist methylthioadenosine 5'-monophosphate. (ox.ac.uk)

In enzymatic assays, utilizing recombinant pol Î· (residues 1-432) proteins, the C34W, I147N, and R167Q variants showed 4- to 14-fold and 3- to 5-fold decreases in specificity constants (kcat/Km) for dATP insertion opposite the 3'-T and 5'-T of a CTD, respectively, compared to the wild-type, while the other variants displayed 2- to 4-fold increases. (bvsalud.org)
Recombinant, human 5-Lipoxygenase expressed in S. fruigiperda insect cells using a baculovirus overexpression system. (sigmaaldrich.com)

In one embodiment, the compound of Formula (I) is (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-yl)phenyl]ethyl}-1,4-oxazepane-2-carboxamide. (justia.com)
In the present study, we used a 5-LOX inhibitor, N- [3-[3-(-fluorophenoxy) phenyl]-1-methyl-2-propenyl]- N -hydroxyurea (BW-B 70C), in a rat model of focal cerebral IR. (biomedcentral.com)

Synthetic peptide derived from the central portion of the ZO-2 protein. (thermofisher.com)

Quatramer™ mediated co-delivery of PI3-Kd/HDAC6 dual inhibitor augments the anti-cancer efficacy of Epirubicin in breast cancer. (harvard.edu)

High levels of intracellular calcium ion activate proteolytic enzymes (known as calpains) that break down many cell proteins, particularly those in the cytoskeleton of neurons (spectrin, neurofilament and microtubule-associated protein). (benbest.com)

Moreover, silencing of S100A11 stimulated mitochondrial superoxide production, which was decreased by AACOCF 3 , as well as N -acetyl- L -cysteine, which also mimicked the effect of PLA 2 inhibitor on NSCLC chemosensitization upon S100A11 silencing. (oncotarget.com)

BMC Cancer (2019) 19:996 Page 2 of 15 PDE-5, PDE-6, PDE-9 are the predominant active iso- Sciences, Naini Allahabad, India. (sagepub.com)

These include biological agents targeting pro-inflammatory cytokines such as interleukin-5 and interleukin-13, inhaled ultra long-acting β 2 -agonists and once daily inhaled corticosteroids. (biomedcentral.com)

The mainstay of treatment for advanced hepatocellular carcinoma (HCC) was the tyrosine kinase inhibitor (TKI) sorafenib [ 5 ]. (biomedcentral.com)

TNF Alpha Inhibitors Market Future Demand And Leading Players Forecast To 2023 - A recent report published by The Business Research Company on TNF Alpha Inhibitors Global Market provides in-depth analysis of segments and sub-segments in the global as well as regional. (powershow.com)

5 Licofelone was developed in order to find compounds with anti-inflammatory activity to obviate the gastrointestinal side-effects related to non-steroidal anti-inflammatory drugs and its safety profile compared to these agents has been authenticated in healthy individuals. (j-epilepsy.org)
Grape seeds represent a low percentage of the fruit weight (about 5% on average), although the antioxidant phenolic compounds present in the seeds account for 60%-70% of the total polyphenols in the grape [10]. (oatext.com)
These regio-specific enzymatic reactions between oxygen and polyunsaturated fatty acids formed new compounds, named oxylipins, which are most frequently with the S-configuration (5-HpETE, 12-HpETE or 15-HpETE). (gerli.com)

Silencing of TSN was accompanied by a significant decrease in S100A11 expression at both mRNA and protein level. (oncotarget.com)
Treatment of murine macrophages (J774A.1) with Mitsui-7 MWCNTsincreased the expression of Alox5 mRNA and protein in a concentration- and time-dependent manner. (cdc.gov)

Immunohistochemical study of brain sections showed IR-mediated increased expression of 5-LOX in the neurons and microglia. (biomedcentral.com)

lipopolysaccharide binding protein [Sourc. (gsea-msigdb.org)

Loss of the tuberous sclerosis complex tumor suppressors triggers the unfolded protein response to regulate insulin signaling and apoptosis. (nih.gov)

LTs exert their biological effects by activating specific receptors belonging to the superfamily of G protein-coupled receptors (GPCRs) [ 22 - 24 ]. (hindawi.com)

Therefore, we designed a protein-free dispersion media containing phospholipids and amino acids in an isotonic balanced electrolyte solution, a solution for nasal and olfactory transport (SNOT). (cdc.gov)

The qualities of grape products are characterized by their metabolic compositions [5,6]. (oatext.com)

Growth control of lung cancer by interruption of 5-lipoxygenase-mediated growth factor signaling. (rush.edu)

Four years later, it was demonstrated, using the Warburg technique for measuring gas exchanges, that proteins present in Lupinus albus seeds were also able to oxidized a variety of fats ( Craig FN, J Biol Chem 1936, 114, 727 ). (gerli.com)

Genes have been cloned for all 5 sub-types and of these, M 1 , M 2 and M 3 receptors have been extensively pharmacologically characterized in animal and human tissue. (justia.com)

It affects 5% of hospitalized patients and has a mortality rate of approximately 50%[ 1 ]. (biomedcentral.com)
Asthma affects 4% to 5% of the US population, a figure that translates into approximately 13 million patients. (respiratory-therapy.com)

The impact of histone deacetylase inhibitors on immune cells and implications for cancer therapy. (harvard.edu)
Leukotriene E4 activates human Th2 cells for exaggerated proinflammatory cytokine production in response to prostaglandin D2. (ox.ac.uk)
However, when combined with PGD(2), cysLTs caused a greater than additive enhancement of the response, with LTE(4) being most effective in activating Th2 cells. (ox.ac.uk)
In HL-60 leukaemia cells, di-GA activated caspase 3 and dose-dependently induced apoptosis. (nature.com)
In unstimulated cells, p50:p65 is sequestered in the cytoplasm by inhibitory proteins known as NF-κB inhibitors (IκBs). (biomedcentral.com)
Studies with bortezomib (VELCADE, formerly known as PS-341) and other proteasome inhibitors indicate that cancer cells are especially dependent on the proteasome for survival, and several mechanisms used by prostate cancer cells require proteasome function. (aacrjournals.org)
ARA55, ARA54, ARA70, BRCA1, and heat-shock proteins) may allow cells to become independent of androgens (intrinsic activation). (aacrjournals.org)
Downregulation of S100A11 by RNAi resulted in enhanced sensitivity of NSCLC cells to cisplatin, oxaliplatin and 5-fluouracil. (oncotarget.com)

aminoguanidine (100 mg/kg, i.p.), as an inducible NOS (iNOS) inhibitor and 7-nitroindazole (60 mg/kg, i.p.), as a neuronal NOS inhibitor were injected 15 min before licofelone. (j-epilepsy.org)
BW-B 70C down-regulated 5-LOX and inhibited iNOS expression by preventing NF-κB activation. (biomedcentral.com)

Repurposing mechanistic insight of PDE-5 inhibitor in cancer chemoprevention through. (sagepub.com)

Anatomy13

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Chemicals and Drugs133

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Phenomena and Processes36

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FLAP8

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Leukotrienes6

Arachidonic acid2

Potent3

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Inhibition4

Cyclooxygenase3

Phosphodiesterase3

Receptor6

Pathway1

Inflammation2

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PPAR2

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Phenyl2

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20191

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20231

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