PLA2SecretoryCytosolic Phospholipase A2VenomSPLA2EnzymeAnnexin A2PeptidesCyclooxygenaseMitogen-activaInhibitionCPLA2PhospholipidsReceptorPotentEnzymesInflammatoryCytoskeletalProteinProstaglandinSelectiveCPLAThromboxaneMonoclonalDepletionActivityArachidonic acidMethylImprovesSignalling pathwayFatty acidsContributesBiologicalSignificantlyActivationActionCurrent
PLA210
- A series of trimethoxyphenyl isoxazolidine derivatives, 5a(i-v) and 5b(i-v), bearing different constituents at the 5th position of the isoxazolidine ring were synthesized and evaluated in vitro and in vivo for their inhibitory activity against purified group I and II phospholipase A2 (PLA2) enzymes from snake venom and human inflammatory synovial fluid. (uni-mysore.ac.in)
- Poultry PM (1.0 mg/ml) caused a significant activation of PLA2 in a time-dependent manner (15-60 min), which was significantly attenuated by the calcium-chelating agents, cPLA2-specific inhibitor (AACOCF3) and antioxidant (vitamin C) in A549 cells. (cdc.gov)
- Phospholipase A2 (PLA2) inhibitors as anti-inflammatory molecules. (uni-mysore.ac.in)
- The interest is in finding alternative specific PLA2 inhibitor(s) from various medicinal plants. (uni-mysore.ac.in)
- Phospholipase A2 (Pla2) is required for memory retrieval, and its inhibition in the hippocampus has been reported to impair memory acquisition in rats. (springer.com)
- Background: The lipoprotein-associated phospholipase A2 inhibitor (Lp-PLA2), rilapladib (SB659032), is being evaluated as a potential treatment to slow the progression of Alzheimer's disease (AD). (cogstate.com)
- Arachidonoyl Thio-PC is a substrate of many phospholipase A2 ( PLA2 ), including sPLA2, cPLA2 and iPLA2. (medchemexpress.com)
- abstract = "In the present study, phospholipase A2 (PLA2) from Lachesis muta (Linnaeus, 1766), is isolated, purified and characterized biochemically and biologically. (edu.pe)
- phospholipase A2, also known as Phosphatidylcholine 2-acylhydrolase 1B, Group IB phospholipase A2, PLA2 and PLA2G1B, is a secreted protein which belongs to thephospholipase A2 family. (betalifesci.com)
- The potential anti-inflammatory activity of these compounds, using bee venom phospholipase A2 (PLA2), was also evaluated. (edu.au)
Secretory2
- Recently, bile acid was found to cause surfactant inactivation by enhancing the activity of secretory phospholipase A2 (sPLA2) and induce inflammatory response of fetal lung [ 5 , 8 ]. (hindawi.com)
- Secreted phospholipase A2 (sPLA2) is a protein secreted by Clonorchis sinensis and is a component of excretory and secretory products ( Cs ESPs). (biomedcentral.com)
Cytosolic Phospholipase A25
- The study was based on the hypothesis that poultry PM would induce the release of inflammatory cytokine interleukin-8 (IL-8) by respiratory epithelial cells under the upstream regulation by cytosolic phospholipase A2 (cPLA2) activation and subsequent formation of cyclooxygenase (COX)- and lipoxygenase (LOX)-catalyzed arachidonic acid (AA) metabolites (eicosanoids). (cdc.gov)
- AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2) . (medchemexpress.com)
- KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 ( cPLA2 or PLA2G4A). (medchemexpress.com)
- Cytosolic phospholipase A2α (cPLA2α), the key enzyme of the arachidonic acid cascade, is considered to be an interesting target for the development of new anti-inflammatory drugs. (bvsalud.org)
- The activation of calcium-dependent cytosolic phospholipase A2 (cPLA2) is involved in inflammatory signaling and is elevated within the plaques of AD brains. (bvsalud.org)
Venom4
- Bothropstoxin-I (BthTx-I) is a Lys49-phospholipase A 2 (Lys49-PLA 2 ) from the venom of Bothrops jararacussu, which despite of the lack of catalytic activity induces myotoxicity, inflammation and pain. (biomedcentral.com)
- Direct electric current from low voltage showed neutralizing properties against venom phospholipase A2 and metalloproteases. (mdpi.com)
- One striking feature of these enzymes is their close homology to venom phospholipases of snakes. (betalifesci.com)
- The potential anti-inflammatory activity of these compounds, using bee venom phospholipase A 2 (PLA 2 ), was also evaluated. (edu.au)
SPLA22
- OBJECTIVES:To evaluate the role of sPLA2 inhibitor Varespladib in mitigating progression of injury. (pcom.edu)
- Surfactant protein A (SP-A) is a main inhibitor of sPLA2 and serves as an integral component of alveolar surfactant consisting of 85~90% phosphatides, 5~10% protein, and 5% sugar [ 9 ]. (hindawi.com)
Enzyme6
- 3-[3-Amino-4-(indan-2-yloxy)-5-(1-methyl-1 H -indazol-5-yl)-phenyl]-propionic acid (AK106-001616) is a novel, potent, and selective inhibitor of the cytosolic phospholipase A 2 (cPLA 2 ) enzyme. (aspetjournals.org)
- Inhibition is substrate-dependent, and the inhibitor likely competes with the substrate for the same binding site of the enzyme. (uni-mysore.ac.in)
- Treatment with multiple therapies (statins, angiotensin converting enzyme [ACE] inhibitor/angiotensin receptor blockers [ARBs], and aspirin) is associated with reduced all-cause mortality. (medscape.com)
- Potent inhibitors of the enzyme include indole-5-carboxylic acids with propan-2-one residues in position 1 of the indole. (bvsalud.org)
- Eight naturally occurring marine-sponge derived sesquiterpenoid quinones were evaluated as potential inhibitors of pyruvate phosphate dikinase (PPDK), a C 4 plant regulatory enzyme. (edu.au)
- On a stable, maximum tolerated labeled dose (at least 4 weeks before screening) of an angiotensin converting enzyme (ACE) inhibitor or angiotensin receptor blocker (ARB), unless documented to be intolerant to ACE inhibitor/ARB. (who.int)
Annexin A211
- Flow cytometric analysis of HL-60 cells (blue) or K562 (green) using Annexin A2 (D11G2) Rabbit mAb (PE Conjugate) (solid lines) or a concentration-matched Rabbit (DA1E) mAb IgG XP ® Isotype Control (PE Conjugate) #5742 (dashed lines). (cellsignal.com)
- Serum annexin A2 levels in patients with colon cancer in comparison to healthy controls and in relation to tumor pathology. (gzsys.org.cn)
- Relationship Between Circulating Tumor Cells and Annexin A2 in Early Breast Cancer Patients. (gzsys.org.cn)
- Association of a characteristic membrane pattern of annexin A2 with high invasiveness and nodal status in colon adenocarcinoma. (gzsys.org.cn)
- Annexin A2 is a molecular target for TM601, a peptide with tumor-targeting and anti-angiogenic effects. (gzsys.org.cn)
- Combined expression of S100A4 and Annexin A2 predicts disease progression and overall survival in patients with urothelial carcinoma. (gzsys.org.cn)
- MIEN1, a novel interactor of Annexin A2, promotes tumor cell migration by enhancing AnxA2 cell surface expression. (gzsys.org.cn)
- Annexin A2: its molecular regulation and cellular expression in cancer development. (gzsys.org.cn)
- Deregulated expression of annexin-A2 and galectin-3 is associated with metastasis in gastric cancer patients. (gzsys.org.cn)
- Annexin A2 depletion delays EGFR endocytic trafficking via cofilin activation and enhances EGFR signaling and metastasis formation. (gzsys.org.cn)
- Annexin A2 positively contributes to the malignant phenotype and secretion of IL-6 in DU145 prostate cancer cells. (gzsys.org.cn)
Peptides2
- In the treatment of High Blood Pressure, the existing ACE inhibitors have side effects and hence, we are attempting to synthesize safe and effective ACE-inhibitory peptides as well as to isolate and characterize ACE inhibitory bioactive molecules from medicinal plant extracts. (uni-mysore.ac.in)
- Annexins do not contain signal peptides, yet some annexins (A1, A2 and A5) appear to be secreted in a physiologically regulated fashion. (assaygenie.com)
Cyclooxygenase4
- Unlike traditional nonsteroidal anti-inflammatory drugs and selective cyclooxygenase-2 inhibitors, AK106-001616 reduced prostaglandin E 2 (PGE 2 ) and leukotriene B 4 (LTB 4 ) production by stimulated cells. (aspetjournals.org)
- 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)
- The high glucose-induced down-regulation of 125 I-Ang II binding was blocked by mepacrine, AACOCF 3 , phospholipase A 2 inhibitors, indomethacin, ibuprofen, and cyclooxygenase inhibitors. (korea.ac.kr)
- Additionally, these drugs, both non-selective inhibitors and selective cyclooxygenase-2 inhibitors, are frequently associated with side effects, impairing patients' compliance to their use 6 . (bvsalud.org)
Mitogen-activa2
- 2002), mitogen-activated protein kinase inhibitors Dacomitinib PD98059 and SB203580 (Lim et al. (phosphorylaseinhibitors.com)
- In addition, the high glucose-induced AA release was blocked by PD 98059, a p44/42 mitogen-activated protein kinase (MAPK) inhibitor. (korea.ac.kr)
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)
- Phospholipase A2 is well known for its role in liver fibrosis and inhibition of tumour cells. (biomedcentral.com)
- However, suppression of the WNT pathway using the acetyltransferase porcupine inhibitor C59 did not reverse EMT whereas a dominant negative form of TCF4 as well as inhibition of phospholipase C using U73122 were able to do so. (cnrs.fr)
- A2 inhibition suppresses ovarian cancer progression via regulating β-catenin/EMT. (gzsys.org.cn)
- These data suggest that increasing cellular levels of cAMP leads to the inhibition of PAF and leukotriene biosynthesis, at least in part, by regulation of phospholipase A 2 activity. (arizona.edu)
CPLA22
- MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2 . (medchemexpress.com)
- FAAH/ cPLA2 α-IN-1 is a dual inhibitor of FAAH and cPLA2α with IC 50 s of 32 and 47 nM, respectively. (medchemexpress.com)
Phospholipids2
- ExoU has phospholipase A2 activity, which can hydrolyze phospholipids such as phosphatidylinositol 4,5-bisphosphate (PIP 2 ). (vt.edu)
- Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. (immune-system-research.com)
Receptor4
- To date, numerous studies have used experimentally induced orofacial inflammation or neuropathy to demonstrate the analgesic properties of a number of novel Inhibitors,research,lifescience,medical compounds: the 5HT1A receptor agonist "type":"entrez-nucleotide","attrs":"text":"F13640″,"term_id":"747767″,"term_text":"F13640″F13640 (Deseure et al. (phosphorylaseinhibitors.com)
- In the current study, the β-adrenergic receptor agonist isoproterenol, alone or in combination with the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (IBMX), was used to increase cAMP in neutrophils. (arizona.edu)
- In 2009, we had a seminal moment when you published a manuscript in The New England Journal of Medicine describing PLA2R, phospholipase A2 receptor, as the antigen that was responsible for a majority of the cases of MN. (medscape.com)
- The M-type phospholipase A2 receptor (PLA2R) in the glomerular podocyte has been identified as the major target antigen in deposited immune-complexes. (msdmanuals.com)
Potent5
- The IC50 value for the most potent interacting inhibitor 5b(v) was 54.8 µM. (uni-mysore.ac.in)
- MAFP is also a potent irreversible inhibitor of anandamide amidase . (medchemexpress.com)
- KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC 50 of 42 nM. (medchemexpress.com)
- Efipladib is a potent, selective and orally active cPLA 2 α inhibitor with an IC 50 of 0.04 μM and a K d of 0.067 μM. (medchemexpress.com)
- Pyrrophenone is a potent and specific cytosolic phospholipase A 2 α ( cPLA 2 α ) inhibitor with an IC 50 value of 4.2 nM. (medchemexpress.com)
Enzymes2
- Mean edematic dose and minimum myotoxic dose were 91.5 mg and 125.89 mg / mL respectively, these values were below enzymes phospholipase A2 from others poisons. (edu.pe)
- Sequences of pancreatic Phospholipase A2 / PLA2G1B enzymes from a variety of mammals have been reported. (betalifesci.com)
Inflammatory1
- The drug studies in rodents have demonstrated that the inflammatory and neuropathic orofacial models can Inhibitors,research,lifescience,medical in some ways be representative of disorders such as TMD and TN and could be used to test new potential treatments. (phosphorylaseinhibitors.com)
Cytoskeletal1
- We have previously demonstrated that Cyclin A2 is involved in cytoskeletal dynamics, epithelial-mesenchymal transition (EMT) and metastasis. (cnrs.fr)
Protein3
- Clara cell 10 (CC10) protein, a homologue of rabbit uteroglobin, is a phospholipase A2 inhibitor. (ihcworld.com)
- Components of the canonical wingless (WNT) pathway, including WNT8b, WNT10a, WNT10b, frizzled 1 and 2 and TCF4 were upregulated at the messenger RNA and protein levels following Cyclin A2 depletion. (cnrs.fr)
- Protein kinase C (PKC) inhibitor blocked high glucose-induced activation of p44/42 MAPK, increase of the [ 3 H]-AA release, and down-regulation of 125 I-Ang II binding. (korea.ac.kr)
Prostaglandin1
- It inhibits prostaglandin synthesis, which prevents formation of platelet-aggregating thromboxane A2. (medscape.com)
Selective1
- GK563 is a selective Ca 2+ -independent phospholipase A 2 ( GVIA iPLA 2 ) inhibitor with an IC 50 value of 1 nM. (medchemexpress.com)
CPLA4
- Tanshinone I is an inhibitor of type IIA human recombinant sPLA 2 ( IC 50 =11 μM) and rabbit recombinant cPLA 2 ( IC 50 =82 μM). (medchemexpress.com)
- Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A 2 (cPLA 2 ) . (medchemexpress.com)
- D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A 2 α ( cPLA 2 α ) activity. (medchemexpress.com)
- ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A 2 α ( cPLA 2 α ) inhibitor , with an IC 50 value of 20 nM. (medchemexpress.com)
Thromboxane1
- Poultry PM also significantly induced the release of COX- and LOX-catalyzed eicosanoids (prostaglandins, thromboxane A2 and leukotrienes B4 and C4) and upstream activation of AA LOX in the cells. (cdc.gov)
Monoclonal1
- Long-term efficacy and downstream mechanism of anti-annexinA2 monoclonal antibody (anti-ANX A2 mAb) in a pre-clinical model of aggressive human breast cancer. (gzsys.org.cn)
Depletion1
- This suggests that a WNT-independent mechanism of beta-catenin activation via phospholipase C is involved in the EMT induced by Cyclin A2 depletion. (cnrs.fr)
Activity1
- Phospholipase A 2 - like activity was assayed in the whole cell by measuring the mobilization of phospholipase A 2 products, PAF, lyso PAF, and arachidonic acid, from cellular phosphoglycerides. (arizona.edu)
Arachidonic acid1
- Inhibitors of arachidonic acid metabolism: effects on rat striatal dopamine release and uptake. (aspetjournals.org)
Methyl1
- Oral supplementation of a diabetogenic diet with the PLA2G1B inhibitor methyl indoxam effectively suppresses diet-induced obesity and diabetes. (betalifesci.com)
Improves1
- By impairing the develop- with specific inhibitors, markedly improves survival in ment of adaptive immune responses needed for recovery, murine sepsis models. (cdc.gov)
Signalling pathway1
- When JNK signalling pathway is blocked by inhibitor SP600125, hepatic stellate cells (HSCs) activation is inhibited, with less proliferation and reduced expression of α-smooth muscle actin (α-SMA) [ 15 ]. (biomedcentral.com)
Fatty acids1
- Phospholipase A2 / PLA2G1B catalyzes the release of fatty acids from glycero-3-phosphocholines. (betalifesci.com)
Contributes1
- Our findings will broaden our knowledge on how Cyclin A2 contributes to EMT and metastasis. (cnrs.fr)
Biological1
- It is used in cell biological experiments as an inhibitor of phospholipase A2. (lookformedical.com)
Significantly1
Activation2
- In Cyclin A2-depleted normal murine mammary gland (NMuMG) cells expressing RasV12, we found that beta-catenin was liberated from the cell membrane and cell-cell junctions and underwent nuclear translocation and activation. (cnrs.fr)
- However, phospholipase A 2 inhibitor did not block high glucose-induced activation of p44/42 MAPK. (korea.ac.kr)
Action1
- 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)
Current1
- In cell cultures, they found that the application of phospholipase A2 inhibitor ONO-RS-082 could increase the current density of two of the three mutant channels tested to non-mutant levels, suggesting a possible therapeutic for some PAH patients. (genomeweb.com)