phospholipase a2 inhibitors
Summary: Compounds that inhibit or block the activity of a PHOSPHOLIPASE A2 enzyme.
Prabhudeva M, Bharath S, Kumar A, Naveen S, Lokanath N, Mylarappa B, et al
. Design and environmentally benign synthesis of novel thiophene appended pyrazole analogues as anti-inflammatory and radical scavenging agents: Crystallographic, in silico modeling, docking and SAR characterization. Bioorg Chem. 2017;73:109-120 pubmed publisher
Lokeshwari D, Achutha D, Srinivasan B, Shivalingegowda N, Krishnappagowda L, Kariyappa A. Synthesis of novel 2-pyrazoline analogues with potent anti-inflammatory effect mediated by inhibition of phospholipase A2: Crystallographic, in silico docking and QSAR analysis. Bioorg Med Chem Lett. 2017;27:3806-3811 pubmed publisher
..Thus, these compounds show promise for development as next-generation nonsteroidal anti-inflammatory drugs. ..
Yun B, Lee H, POWELL R, Reisdorph N, Ewing H, Gelb M, et al
. Regulation of calcium release from the endoplasmic reticulum by the serine hydrolase ABHD2. Biochem Biophys Res Commun. 2017;490:1226-1231 pubmed publisher
..The results describe a novel mechanism for regulating calcium transfer from the endoplasmic reticulum to mitochondria that involves the serine hydrolase ABHD2. ..
Lindholm D, Lindback J, Armstrong P, Budaj A, Cannon C, Granger C, et al
. Biomarker-Based Risk Model to Predict Cardiovascular Mortality in Patients With Stable Coronary Disease. J Am Coll Cardiol. 2017;70:813-826 pubmed publisher
..The Stabilization of Atherosclerotic Plaque by Initiation of Darapladib Therapy Trial [STABILITY]; NCT00799903). ..
White H, Held C, Stewart R, Tarka E, Brown R, Davies R, et al
. Darapladib for preventing ischemic events in stable coronary heart disease. N Engl J Med. 2014;370:1702-11 pubmed publisher
..Funded by GlaxoSmithKline; STABILITY ClinicalTrials.gov number, NCT00799903.). ..
Yeo A, Li L, Warren L, Aponte J, Fraser D, King K, et al
. Pharmacogenetic meta-analysis of baseline risk factors, pharmacodynamic, efficacy and tolerability endpoints from two large global cardiovascular outcomes trials for darapladib. PLoS ONE. 2017;12:e0182115 pubmed publisher
Vieira S, Da Rocha S, Neves Ferreira A, Almeida R, Perales J. Heterologous expression of the antimyotoxic protein DM64 in Pichia pastoris. PLoS Negl Trop Dis. 2017;11:e0005829 pubmed publisher
..rDM64 formed a noncovalent complex with myotoxin II (Lys49-PLA2) from Bothrops asper and displayed biological activity that was similar to that of native DM64, inhibiting the cytotoxicity of myotoxin II by 92% at a 1:1 molar ratio. ..