prostaglandin-h2 and thiobarbituric-acid

prostaglandin-h2 has been researched along with thiobarbituric-acid* in 1 studies

Other Studies

1 other study(ies) available for prostaglandin-h2 and thiobarbituric-acid

Article	Year
A facilitated approach to evaluate the inhibitor mode and potency of compounds targeting microsomal prostaglandin e synthase-1. Assay and drug development technologies, 2011, Volume: 9, Issue:5 Microsomal prostaglandin E(2) synthase-1 (MPGES1) catalyzes the formation of prostaglandin E(2) from the endoperoxide prostaglandin H(2). MPGES1 expression is induced in inflammatory diseases, and this enzyme is regarded as a potential drug target. To aid in the drug discovery effort, a simple method for determination of inhibition mechanism and potency toward both prostaglandin H(2) and glutathione (GSH) has been developed. Using an assay with thiobarbituric acid-based detection, the inhibitory effects of six MPGES1 inhibitors were evaluated. The IC(50) values obtained at three substrate (S) concentrations ([S]K(M)) were used to estimate inhibition modality and inhibition constant values. This facilitated strategy is a useful and general screening method to evaluate the inhibitory effects of new drug compounds. Topics: Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Drug Interactions; Enzyme Inhibitors; Fluorescence; Glutathione; Humans; Indoles; Inhibitory Concentration 50; Intramolecular Oxidoreductases; Malondialdehyde; Models, Theoretical; Molecular Targeted Therapy; Pharmacokinetics; Prostaglandin H2; Prostaglandin-E Synthases; Thiobarbiturates	2011

Article

Year

A facilitated approach to evaluate the inhibitor mode and potency of compounds targeting microsomal prostaglandin e synthase-1.

Assay and drug development technologies, 2011, Volume: 9, Issue:5

Microsomal prostaglandin E(2) synthase-1 (MPGES1) catalyzes the formation of prostaglandin E(2) from the endoperoxide prostaglandin H(2). MPGES1 expression is induced in inflammatory diseases, and this enzyme is regarded as a potential drug target. To aid in the drug discovery effort, a simple method for determination of inhibition mechanism and potency toward both prostaglandin H(2) and glutathione (GSH) has been developed. Using an assay with thiobarbituric acid-based detection, the inhibitory effects of six MPGES1 inhibitors were evaluated. The IC(50) values obtained at three substrate (S) concentrations ([S]K(M)) were used to estimate inhibition modality and inhibition constant values. This facilitated strategy is a useful and general screening method to evaluate the inhibitory effects of new drug compounds.

Topics: Dose-Response Relationship, Drug; Drug Discovery; Drug Evaluation, Preclinical; Drug Interactions; Enzyme Inhibitors; Fluorescence; Glutathione; Humans; Indoles; Inhibitory Concentration 50; Intramolecular Oxidoreductases; Malondialdehyde; Models, Theoretical; Molecular Targeted Therapy; Pharmacokinetics; Prostaglandin H2; Prostaglandin-E Synthases; Thiobarbiturates

2011