2010
DOI: 10.1016/j.ejmech.2009.10.025
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Identification and characterisation of new inhibitors for the human hematopoietic prostaglandin D 2 synthase

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Cited by 18 publications
(9 citation statements)
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“…The inhibition of GSTs has been extensively studied in vitro and the following compounds from plants have been found to be inhibitors of the enzymes: tannic acid, thonningianin A, cibacron blue, hematin, ethacrynic acid, ellagic acid, ferulic acid, caffeic acid, stilbene, quercetin, chlorogenic acid and curcumin have been long reported by many researchers [ 61 64 ]. Ethacrynic acid binds to the H-site of GSTs but has low affinity for the enzyme, and conjugated with GSH, it is easily excreted from the cell.…”
Section: Discussionmentioning
confidence: 99%
See 1 more Smart Citation
“…The inhibition of GSTs has been extensively studied in vitro and the following compounds from plants have been found to be inhibitors of the enzymes: tannic acid, thonningianin A, cibacron blue, hematin, ethacrynic acid, ellagic acid, ferulic acid, caffeic acid, stilbene, quercetin, chlorogenic acid and curcumin have been long reported by many researchers [ 61 64 ]. Ethacrynic acid binds to the H-site of GSTs but has low affinity for the enzyme, and conjugated with GSH, it is easily excreted from the cell.…”
Section: Discussionmentioning
confidence: 99%
“…The IC 50 values of P. curatellifolia ethanol extracts on the kidney GSTs and of the aqueous extracts on both the liver and the kidney GSTs were higher than those of ETA, a standard GST inhibitor indicating that this extract was an effective inhibitor. GST Sigma (hematopoietic prostaglandin D 2 synthase H-PGDS,) is involved in inflammation by its role in the isomerisation of PGH 2 to produce PGD2, which is an allergic mediator and promotes the inflammatory process [ 64 ]. H-PGDS is, thus, a target for the design of anti-inflammatory and anti-allergic drugs.…”
Section: Discussionmentioning
confidence: 99%
“…Screening of a range of GST inhibitors showed that tetrazole 168 (Figure 15) and Cibacron Blue 3G-A (176, Figure 15) were the most potent inhibitors of hPGDS (IC 50 ¼ 0.2-1.8 lM) (Weber et al 2010). Characterization of the inhibition of hPGDS by nocodazole (177, Figure 15) (IC 50 %65 lM) by docking calculations indicated binding at the prostaglandin H-site.…”
Section: Theta-class (Gstt)mentioning
confidence: 99%
“…However, since 15‐lipoxygenase overexpression in alveolar macrophages is clearly confined to the Th2‐high phenotype of asthma (53, 76), it is possible that sub‐phenotype differences in leukotriene antagonist response will be observed in future studies. Furthermore, emerging strategies for the treatment of asthma include the development of inhibitors of prostaglandin D2 and its receptor (77–80). Whether patient selection for therapies targeting eicosanoids should be based on molecular phenotypes will be important in the clinical evaluation of these agents and requires further study as well.…”
Section: Treatment Implications Of Asthma Phenotypesmentioning
confidence: 99%