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Structure-based, multi-targeted drug discovery approach to eicosanoid inhibition: Dual inhibitors of

Journal Article · · BBA - General Subjects

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1767217
Journal Information:
BBA - General Subjects, Vol. 1865, Issue (2)
Country of Publication:
United States
Language:
ENGLISH

References (39)

The eicosanoids and their biochemical mechanisms of action journal April 1989
Prostanoids in health and disease: Fig. 1. journal December 2008
Prostaglandins and Leukotrienes: Advances in Eicosanoid Biology journal November 2001
Prostaglandins and Inflammation journal May 2011
The Coxibs, Selective Inhibitors of Cyclooxygenase-2 journal August 2001
Risk of Cardiovascular Events Associated With Selective COX-2 Inhibitors journal August 2001
Role of Prostacyclin in the Cardiovascular Response to Thromboxane A2 journal April 2002
Characterization of Microsomal Prostaglandin E Synthase 1 Inhibitors journal November 2013
Cyclooxygenases, microsomal prostaglandin E synthase-1, and cardiovascular function journal May 2006
Biosynthesis and metabolism of leukotrienes journal July 2007
Leukotrienes journal November 2007
The membrane organization of leukotriene synthesis journal April 2004
Effects of a FLAP inhibitor, GSK2190915, in asthmatics with high sputum neutrophils journal February 2014
Initial Clinical Experience with AZD5718, a Novel Once Daily Oral 5-Lipoxygenase Activating Protein Inhibitor: Initial Clinical Experience with AZD5718 journal March 2018
Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease journal March 2019
Discovery of the first dual inhibitor of the 5-lipoxygenase-activating protein and soluble epoxide hydrolase using pharmacophore-based virtual screening journal February 2017
Discovery of Novel 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors by Exploiting a Multistep Virtual Screening Protocol journal February 2020
Targeting biosynthetic networks of the proinflammatory and proresolving lipid metabolome journal February 2019
Dual Acting Anti-Inflammatory Drugs journal February 2007
Licofelone Suppresses Prostaglandin E 2 Formation by Interference with the Inducible Microsomal Prostaglandin E 2 Synthase-1 journal June 2008
Licofelone-A Novel Analgesic and Anti-Inflammatory Agent journal February 2007
The molecular mechanism of the inhibition by licofelone of the biosynthesis of 5-lipoxygenase products: Licofelone and 5-lipoxygenase product synthesis journal October 2007
Protective effects of licofelone, a 5-lipoxygenase and cyclo-oxygenase inhibitor, versus naproxen on cartilage loss in knee osteoarthritis: a first multicentre clinical trial using quantitative MRI journal July 2008
Licofelone--clinical update on a novel LOX/COX inhibitor for the treatment of osteoarthritis journal February 2004
Dynamic eicosanoid responses upon different inhibitor and combination treatments on the arachidonic acid metabolic network journal January 2012
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors journal December 2015
Bioinformatic and enzymatic characterization of the MAPEG superfamily: Characterization of MAPEG members journal March 2005
Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886 journal July 2005
Identification of multi-target inhibitors of leukotriene and prostaglandin E2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7 journal April 2018
Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity journal May 2020
BRP-187: A potent inhibitor of leukotriene biosynthesis that acts through impeding the dynamic 5-lipoxygenase/5-lipoxygenase-activating protein (FLAP) complex assembly journal November 2016
Crystal Structure of Inhibitor-Bound Human 5-Lipoxygenase-Activating Protein journal July 2007
Crystal structure of microsomal prostaglandin E2 synthase provides insight into diversity in the MAPEG superfamily journal February 2013
Crystallizing Membrane Proteins in the Lipidic Mesophase. Experience with Human Prostaglandin E2 Synthase 1 and an Evolving Strategy journal March 2014
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics journal May 2015
Discovery and characterization of [(cyclopentyl)ethyl]benzoic acid inhibitors of microsomal prostaglandin E synthase-1 journal March 2017
5-Lipoxygenase-Activating Protein (FLAP) Inhibitors. Part 4: Development of 3-[3- tert -Butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1 H -indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor journal December 2011
The Minimum Significant Ratio: A Statistical Parameter to Characterize the Reproducibility of Potency Estimates from Concentration-Response Assays and Estimation by Replicate-Experiment Studies journal April 2006
Identification and Characterization of Novel Microsomal Prostaglandin E Synthase-1 Inhibitors for Analgesia journal January 2016