Last update 01 Nov 2024

5-LOX x TXA2 synthase

Last update 01 Nov 2024

Basic Info

Related Targets

5-LOXTXA2 synthase

Drugs associated with 5-LOX x TXA2 synthase

E-6700

Target

5-LOX x TXA2 synthase

Mechanism

5-LOX inhibitors [+1]

Active Org.-

Originator Org.

Eisai Co., Ltd.

Active Indication-

Inactive Indication

Asthma

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

CV-6504

Target

5-LOX x TXA2 synthase

Mechanism

5-LOX inhibitors [+1]

Active Org.-

Originator Org.

Takeda Pharmaceutical Co., Ltd.

Active Indication-

Inactive Indication

Nephritis [+1]

Drug Highest PhaseDiscontinued

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

NIK-639

Target

5-LOX x TXA2 synthase

Mechanism

5-LOX inhibitors [+1]

Active Org.-

Originator Org.

Kowa Co., Ltd.

Active Indication-

Inactive Indication

Asthma

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with 5-LOX x TXA2 synthase

100 Translational Medicine associated with 5-LOX x TXA2 synthase

0 Patents (Medical) associated with 5-LOX x TXA2 synthase

Literatures (Medical) associated with 5-LOX x TXA2 synthase

01 Jan 2024·Journal of Ethnopharmacology

Multi-omics approaches revealed the therapeutic mechanisms of Suo-Quan-Wan for treating overactive bladder in spontaneously hypertensive rats

Article

Author: Wu, Yushan ; Xu, Pingxiang ; Cheng, Mingchang ; Xue, Ming ; Tie, Yan ; Sun, Zhihui ; Zhou, Xuelin ; Xu, Liping ; Tong, Xinyi

ETHNOPHARMACOLOGICAL RELEVANCESuo-Quan-Wan (SQW), a traditional Chinese prescription, has been used for hundreds of years to alleviate overactive bladder (OAB) symptoms such as frequent and nocturnal urination. However, limited modern research on OAB therapeutic targets has hindered the use and development of SQW.AIM OF THE STUDYThis study aimed to investigate the biological mechanisms and key targets of SQW on OAB in spontaneously hypertensive rats (SHR) using an integrated analysis of network pharmacology, transcriptome and metabolome.METHODSRats were divided into five groups: model group (SHR), control group (WKY), darifenacin group, high dose (SQWH) and low dose (SQWL) group. Urodynamic parameters and histological examination were detected. Network pharmacology, transcriptome, and metabolome were used to screen for disease gene targets, differential mRNA, and differential metabolites, respectively. The biological targets and mechanisms of SQW for OAB were analyzed. Western blotting was performed to verify the proteins of key differential targets.RESULTSUrodynamics revealed a significant decrease in storage parameters in SHR. After SQW treatment, the inter-contraction interval, voided volume and bladder capacity increased by 2-3 times, as well as bladder compliance. Additionally, SQW improved the pathological changes in the urinary tract epithelium and the detrusor layer of the bladder in SHR. Metabolomic results showed an increase in arachidonic acid (AA) and cyclic adenosine monophosphate (cAMP) in plasma, suggesting the involvement of arachidonic acid metabolism and purine metabolism in SQW treatment. The downregulation of cytochrome P450 1B1 (CYP1B1), thromboxane-A synthase (TBXAS1), polyunsaturated fatty acid 5-lipoxygenase (ALOX5), and cAMP-specific 3',5'-cyclic phosphodiesterase 4B (PDE4B) were confirmed through topological analysis and Venn analysis of omics data and network pharmacology. These proteins affected the metabolism of AA and cAMP, respectively, and consequently affected downstream proteins, such as transient receptor potential (TRP) cation channel proteins (e.g. TRPV1, TRPA1, and TRPM8), myosin light chain kinase (MLCK), and the phosphorylation of myosin regulatory light chain (p-MLC).CONCLUSIONThis study initially elucidated the importance of AA and cAMP in the treatment of SQW, indicating the AA-CYP1B1/TBXAS1/ALOX5-TRPA1/TRPV1/TRPM8 and cAMP-PDE4B-MLCK-p-MLC pathways as the important pathways in SQW-treated SHR bladder in vivo.

01 Aug 2021·Prostaglandins & Other Lipid MediatorsQ3 · BIOLOGY

Evaluation of inhibitors of the arachidonic acid cascade with intact platelets using an on-line dilution and on-line solid phase extraction HPLC–MS method

Q3 · BIOLOGY

Article

Author: Fabian, Jörg ; Mergemeier, Kira ; Lehr, Matthias

An automatic on-line dilution/on-line solid phase extraction (SPE) system has been developed for the detection of metabolites of the arachidonic acid cascade in platelets. The method allows the direct injection of larger quantities of centrifugates from cell suspensions previously treated with an equal volume of an acetonitrile/methanol mixture for protein precipitation. The method was used to study the effect of inhibitors of platelet arachidonic acid cascade enzymes (cytosolic phospholipase A₂α, cyclooxygenase-1, thromboxane synthase, 12-lipoxygenase) and related targets (cyclooxygenase-2, microsomal prostaglandin E synthase-1, 5-lipoxygenase) in intact platelets after stimulation with calcium ionophore A23187. In addition to enzyme inhibition, the cell-damaging properties of the test compounds was determined by measuring the release of serotonin from the platelets into the incubation buffer.

02 Apr 2019·Journal of Investigational Allergology and Clinical ImmunologyQ3 · MEDICINE

Angioedema-Induced by Nonsteroidal Anti-inflammatory Drugs: A Genotype-Phenotype Correlation in A Brazilian Population

Q3 · MEDICINE

Article

Author: Sole, D ; Filippelli-Silva, R ; Veronez, C L ; Pesquero, J B ; Martin, R P ; Ensina, L F

This paper discusses about the angioedema-induced by nonsteroidal anti-inflammatory drugs, genotype-phenotype correlation in Brazilian population.Nonsteroidal anti-infammatory drugs (NSAIDs) are the leading cause of hypersensitivity reactions in Latin America, both in adults and children.Therefore, in this study, we used whole-exome sequencing (WES) to detect genetic markers.That determine a hypersensitivity response in patients with NSAID-induced isolated angioedema (NIA).Four unrelated patients with NIA and their parents were selected and agreed to participate in the study.Nine genes related to the COX and 5-LO signaling pathways (ALOX5, PTGS2, CYSLTR1, CYSLTR2, LTC4S, PTGER1, PTGER2, TBXA2R, TBXAS1) were filtered in the VCF file according to variant segregation anal. in order to propose the genotype-phenotype associationTaken together, our data enable us to conclude that there is probably no single genetic marker of NIA in our cohort of patients.NIA is most likely determined by a combination of genetic alterations.

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