Leukotriene synthesis inhibitorsInhibitionPathwaysArachidonic acid metabEnzymesPhospholipase A2 inhibitorBiosynthesisNordihydroguaiaretic acidCyclooxygenase inhibitorsLeukotrienesSelectiveZileutonAspirinInflammationReceptorNSAIDsPharmacologyAntineoplasticPathwayCelecoxibInducesInhibitoryMoleculeIC50Anti-inflammatoryMechanismReceptorsInteractionDerivativesMechanismsActivityEffectEffectsDualDrugGrowthCancer cellCellResponse
Leukotriene synthesis inhibitors3
- Antileukotrienes include leukotriene receptor antagonists (e.g. montelukast, zafirlukast and pranlukast) and leukotriene synthesis inhibitors (e.g. zileuton) [6]. (roma2024.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)
- however, studies provide some data on leukotriene synthesis inhibitors as possible therapeutic agents for patients with Sjögren-Larsson syndrome. (medscape.com)
Inhibition5
- However, the results also suggest that certain inhibitors of arachidonic acid metabolism are relatively potent DA uptake blockers/releasers and that this action is unrelated to their inhibition of enzymes in the arachidonic acid cascade. (aspetjournals.org)
- 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)
- The data indicated that inhibition of the cyclooxygenase pathway alone was less effective than inhibition of both the lipoxygenase and cyclooxygenase pathways of arachidonic- acid metabolism in blocking A23187 mediated chemiluminescence. (cdc.gov)
- 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)
- It has been shown to induce an anti-inflammatory effect, possibly through inhibition of the enzymes 5-lipoxygenase and cyclooxygenase inflammation pathways. (keystobasichealth.com)
Pathways3
- The prostaglandin and leukotriene families of lipid mediators are formed via two distinct biosynthetic pathways that are initiated by the oxygenation of arachidonic acid by either cyclooxygenase-2 (COX-2) or 5-lipoxygenase (5-LOX), respectively. (elsevierpure.com)
- We aimed at evaluating whether combined blocking of the COX-2 and 5-LOX pathways might have additive antitumor effects in colorectal cancer. (unifi.it)
- The pathogenesis of AIA has implicated both the lipoxygenase (LO) and the cyclooxygenase (COX) pathways. (medscape.com)
Arachidonic acid metab2
- Inhibitors of arachidonic acid metabolism: effects on rat striatal dopamine release and uptake. (aspetjournals.org)
- Cyclooxygenase (COX)-2 and 5-lipoxygenase (5-LOX) are key enzymes involved in arachidonic acid metabolism. (unifi.it)
Enzymes4
- Nordihydroguaiaretic acid is an antioxidant, and it may block certain enzymes needed for tumor growth. (wikipedia.org)
- It is also a lipoxygenase inhibitor that helps block enzymes responsible for inflammation. (kitchen-prescription.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)
- Urtica dioica contains powerful phytonutrients that also block both the 5-alpha reductase and aromatase enzymes, providing another safeguard to keep your important testosterone from converting to DHT or estrogen. (keystobasichealth.com)
Phospholipase A2 inhibitor2
- U-73122 (10 microM), another phospholipase A2 inhibitor, decreased evoked overflow of DA, did not affect the action of N-0437 but also increased spontaneous outflow of DA. (aspetjournals.org)
- The phospholipase-A2 inhibitor, quinacrine, completely blocked A23187 induced chemiluminescence but only partially blocked FMLP stimulated chemiluminescence. (cdc.gov)
Biosynthesis2
- HKD2 and HKE2 were formed in human blood leukocytes activated with bacterial lipopolysaccharide and calcium ionophore A23187, and biosynthesis was blocked by inhibitors of 5-LOX or COX-2. (elsevierpure.com)
- DL-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis . (abmole.com)
Nordihydroguaiaretic acid2
- This study investigated the contribution of lipoxygenase (LOX) inhibitors, nordihydroguaiaretic acid (NDGA), tetra-O-methyl nordihydroguaiaretic acid (M4N) and zileuton (ZIL), and thromboxane A2 (TXA2) inhibitor 4,5-diphenylimidazole (DPI) in the proliferation of Brucella abortus infection. (gnu.ac.kr)
- In slices prelabeled with [3H]DA, exposure to BPB, U-73122 and nordihydroguaiaretic acid (a lipoxygenase inhibitor) significantly increased spontaneous outflow of tritium whereas the cyclooxygenase inhibitors aspirin and indomethacin did not. (aspetjournals.org)
Cyclooxygenase inhibitors1
- 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)
Leukotrienes3
- Leukotrienes result from the action of 5-lipoxygenase on arachidonic acid and are synthesized by a variety of inflammatory cells in the airways, including eosinophils, mast cells, macrophages, and basophils. (brainkart.com)
- Trials with leukotriene inhibitors have demonstrated an important role for leukotrienes in aspirin-induced asthma. (brainkart.com)
- Antileukotriene receptor antagonists (LTR As) bind competitively to cysteinyl leukotriene receptors 1 and block the contractile advertising activity of leukotrienes in airway clean muscles. (roma2024.com)
Selective10
- Cyclooxygenase-2 (COX-2) is the molecular target of non-steroidal anti-inflammatory drugs (NSAIDs) and selective COX-2 inhibitors. (vanderbilt.edu)
- PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively. (dcchemicals.com)
- A-908292 is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 38 nM (hACC2), no activity against ACC1 (IC50>30 uM). (dcchemicals.com)
- ACC2 inhibitor 2e is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 1.9 nM and 1950 nM for ACC2 and ACC1, respectively.ACC2 inhibitor 2e exhibited good PK profile and in vivo antidiabetic efficacy in C57BL/6 mice. (dcchemicals.com)
- Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of ferroptosis with EC50 of 60 nM. (abmole.com)
- Erastin2 is a ferroptosis inducer and a potent, selective inhibitor of the system xc(-) cystine/glutamate transporter. (abmole.com)
- IFSP1 is an effective, selective and glutathione-independent inhibitor of ferroptosis Suppressor protein 1 (FSP1/AIFM2) with an EC50 value of 103 nM. (abmole.com)
- It is also a potent, selective, and metabolically stable system XC -- inhibitor. (abmole.com)
- UAMC-3203 hydrochloride is a potent and selective Ferroptosis inhibitor, with an IC50 of 12 nM. (abmole.com)
- PD 146176 is a selective 15-lipoxygenase inhibitor. (abmole.com)
Zileuton1
- zileuton, a 5-lipoxygenase inhibitor, and zafirlukast and montelukast, LTD 4 -receptor antagonists. (brainkart.com)
Aspirin4
- Support for this idea was provided by the demonstration that leukotriene pathway inhibitors impressively reduce the response to aspirin challenge and improve overall control of asthma on a day-to-day basis. (brainkart.com)
- The limited anti-thrombotic efficacy of aspirin may reflect the fact that it blocks only one source of ADP which is that released in a thromboxane-dependent manner following platelet adhesion (see e.g. (justia.com)
- LT-modifying drugs are effective in blocking the bronchoconstriction provoked by aspirin and are used in the treatment of this condition. (medscape.com)
- Further investigations by Smith concluded that aspirin and indomethacin inhibited synthesis by specifically blocking oxygenation of arachidonic acid. (medscape.com)
Inflammation2
- 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)
- Curcumin works on a molecular level by blocking NF-kB, a molecule that is believed to play a major role in inflammation and many chronic diseases. (amandean.com)
Receptor4
- DPI treatment showed reduced survival of Brucella at 24 h post-incubation while blocking LTB4 receptor was observed to have a lower intracellular growth at 48 h post-incubation suggesting different action of the inhibitors in the course of the survival of Brucella within the cells. (gnu.ac.kr)
- 10 microM) increased electrically evoked overflow of endogenous DA from rat striatal slices and appeared to partially block the modulatory effects of the D-2 DA receptor agonist N-0437 on this release. (aspetjournals.org)
- In addition, drugs that block components of the arachidonic acid pathway that targets neutrophilic asthma and CRTH2 receptor antagonists that inhibit the proinflammatory actions of prostaglandin D 2 may become available. (biomedcentral.com)
- Adverse Effects of Repeated, Intravenous Morphine on Recovery after Spinal Cord Injury in Young, Male Rats Are Blocked by a Kappa Opioid Receptor Antagonist. (tamu.edu)
NSAIDs2
- Foremost among these are non-steroidal anti-inflammatory drugs (NSAIDs) and cyclooxygenase-2 (COX-2) inhibitors. (vanderbilt.edu)
- The safety of the use of bromelain compared to other anti-inflammatories, derives from the difference in its mechanism of action: in fact, where NSAIDs inhibit cyclooxygenase, blocking the synthesis of prostaglandins, bromelain, instead, increases the production of prostaglandins with anti-inflammatory activity detrimental to those with pro-inflammatory activity: thus the gastrointestinal damage typical of NSAIDs is avoided. (nutrami.it)
Pharmacology1
- The Pharmacology of TNF Inhibitors - August 17, 2001. (powershow.com)
Antineoplastic1
- The administration of the ceramide synthase inhibitor fumonisin B1 could prevent some of these antineoplastic effects. (unifi.it)
Pathway4
- This study describes an integrated pathway in beta cells that links beta cell dysfunction induced by pro-inflammatory cytokines with 12-lipoxygenase and NADPH oxidase (NOX-1) activation. (nih.gov)
- Inhibitors of this pathway may provide a new therapeutic strategy to preserve beta cell mass in diabetes. (nih.gov)
- docs.gogle.com/list of NF-kB pathway inhibitors. (transcendingsquare.com)
- Supplementation with flavonoids can block this from occurring by inhibiting an earlier step in the intracellular pathway by preventing the stimulation of the IKK complex and the translocation of NF-κB into the cell nucleus where the pro-inflammatory cytokines are made. (transcendingsquare.com)
Celecoxib2
- The effects of the COX-2 inhibitor celecoxib and the 5-LOX inhibitor MK886 on prostaglandin E(2) and cysteinyl leukotriene production,tumor cell proliferation,cell apoptosis,and Bcl-2/Bax expression were evaluated in the Caco-2 and HT29 colon cancer cells. (unifi.it)
- Combined treatment with 10 micromol/L celecoxib and MK886 could prevent this activation and had additive effects on inhibiting tumor cell proliferation,inducing cell apoptosis,decreasing Bcl-2 expression,increasing Bax expression,and determining mitochondrial depolarization in comparison with treatment with either inhibitor alone. (unifi.it)
Induces2
- It has previously been reported that pro-inflammatory cytokine stimulation induces 12-lipoxygenase (12-LO) expression in human islets. (nih.gov)
- ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor that induces iron death and has shown cytotoxic effects against melanoma, lung adenocarcinoma, fibrosarcoma, and pancreatic cancer cell lines. (abmole.com)
Inhibitory1
- Apigenin: Found in most species of Chamomile, the flavone apigenin is also a safe and effective aromatase inhibitor, with an inhibitory effectiveness about equal to chrysin. (keystobasichealth.com)
Molecule1
- This includes lipoxygenases, which incorporate one molecule of O2 into the carbon framework and cyclooxygenases, which incorporate two molecules of O2. (vanderbilt.edu)
IC501
- UAMC-3203 is an improved ferroptosis inhibitor, with an IC50 value of 10 nM in IMR-32 neuroblastoma cells. (abmole.com)
Anti-inflammatory2
- We are exploiting this discovery to prepare novel COX-2 inhibitors as anti-inflammatory drugs and cancer preventive agents. (vanderbilt.edu)
- Boswellic acid is made up of four main anti-inflammatory acids that are inhibitors of 5-lipoxygenase (5-LO), an enzyme that produces leukotriene. (amandean.com)
Mechanism1
- The mechanism may be related to the blocking of the MPTP opening and the subsequent reduction of Cyt C release. (geneticsmr.com)
Receptors1
- Because of the evidence of leukotriene involvement in many inflammatory diseases and in anaphylaxis, consid-erable effort has been expended on the development of drugs that block the synthesis of these arachidonic acid derivatives or their receptors. (brainkart.com)
Interaction1
- Our laboratory has combined structural analysis with functional studies to define the molecular determinants of the interaction of ligands (substrates and inhibitors) with COX-2. (vanderbilt.edu)
Derivatives1
- Comparative analysis of the effect of site-directed mutation of active site residues on the binding of substrates and inhibitors to COX-1 and COX-2 led us to hypothesize that neutral derivatives of esters and amides would bind selectively to COX-2. (vanderbilt.edu)
Mechanisms1
- 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)
Activity1
- Compounds that inhibit or block the PHOSPHATASE activity of CALCINEURIN. (bvsalud.org)
Effect1
- JKE-1674 reduces viability of LOX-IMVI cancer cells and in a panel of additional cancer cell lines, an effect that can be blocked by the ferroptosis inhibitor ferrostatin-1. (abmole.com)
Effects1
- Nor-Binaltorphimine Blocks the Adverse Effects of Morphine after Spinal Cord Injury. (tamu.edu)
Dual2
- PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. (dcchemicals.com)
- The dual cyclooxygenase/5-lipoxygenase inhibitor licofelone attenuates p-glycoprotein-mediated drug resistance in the injured spinal cord. (tamu.edu)
Drug1
- A23187 induced chemiluminescence was inhibited by the calmodulin inhibitor, R24571, and the antiinflammatory drug, MK830. (cdc.gov)
Growth1
- 3. may help treat or even prevent prostate cancer by blocking male hormones that encourage the growth of prostate cancer cells, according to preliminary laboratory research at the Mayo Clinic. (keystobasichealth.com)
Cancer cell1
- Furthermore, di-GA inhibited the generation of lymphendothelial gaps by cancer cell spheroid-secreted lipoxygenase metabolites. (nature.com)
Cell2
- TNF inhibitors may increase the risk of skin cancer, particularly non-melanoma skin cancers like squamous cell carcinoma. (powershow.com)
- Liproxstatin-1 is a potent inhibitor of ferroptosis, a non-apoptotic form of cell death characterized by iron-dependent accumulation of lethal lipid reactive oxygen species (ROS). (abmole.com)
Response1
- PURPOSE/OBJECTIVE(S): Most patients with metastatic colorectal cancer (CRC) have microsatellite stable (MSS) disease with a limited response to immune checkpoint inhibitors (ICIs). (bvsalud.org)