Structure-based, multi-targeted drug discovery approach to eicosanoid inhibition: Dual inhibitors of mPGES-1 and 5-lipoxygenase activating protein (FLAP)

Discovery of Novel 5-Lipoxygenase-Activating Protein (FLAP) Inhibitors by Exploiting a Multistep Virtual Screening Protocol

(2020) Abdurrahman Olgac et al.   Journal of Chemical Information and Modeling

Encapsulation of the dual FLAP/mPEGS-1 inhibitor BRP-187 into acetalated dextran and PLGA nanoparticles improves its cellular bioactivity

(2020) Blerina Shkodra-Pula et al.   JOURNAL OF NANOBIOTECHNOLOGY

Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease

(2019) Daniel Pettersen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting biosynthetic networks of the proinflammatory and proresolving lipid metabolome

(2019) Markus Werner et al.   FASEB JOURNAL

Initial Clinical Experience with AZD5718, a Novel Once Daily Oral 5-Lipoxygenase Activating Protein Inhibitor

(2018) Hans Ericsson et al.   CTS-Clinical and Translational Science

Identification of multi-target inhibitors of leukotriene and prostaglandin E 2 biosynthesis by structural tuning of the FLAP inhibitor BRP-7

(2018) Zehra Tuğçe Gür et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the first dual inhibitor of the 5-lipoxygenase-activating protein and soluble epoxide hydrolase using pharmacophore-based virtual screening

(2017) Veronika Temml et al.   Scientific Reports

BRP-187: A potent inhibitor of leukotriene biosynthesis that acts through impeding the dynamic 5-lipoxygenase/5-lipoxygenase-activating protein (FLAP) complex assembly

(2016) Ulrike Garscha et al.   BIOCHEMICAL PHARMACOLOGY

Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors

(2015) Matthew A. Schiffler et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics

(2015) John Gately Luz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Crystallizing Membrane Proteins in the Lipidic Mesophase. Experience with Human Prostaglandin E2 Synthase 1 and an Evolving Strategy

(2014) Dianfan Li et al.   CRYSTAL GROWTH & DESIGN

Characterization of Microsomal Prostaglandin E Synthase 1 Inhibitors

(2013) Marina Korotkova et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Crystal structure of microsomal prostaglandin E2 synthase provides insight into diversity in the MAPEG superfamily

(2013) T. Sjogren et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of a FLAP inhibitor, GSK2190915, in asthmatics with high sputum neutrophils

(2013) R. Chaudhuri et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Dynamic eicosanoid responses upon different inhibitor and combination treatments on the arachidonic acid metabolic network

(2012) Chong He et al.   Molecular BioSystems

Prostaglandins and Inflammation

(2011) Emanuela Ricciotti et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

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)-1H-indol-2-yl]-2,2-dimethylpropionic Acid (AM803), a Potent, Oral, Once Daily FLAP Inhibitor

(2011) Nicholas S. Stock et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2008) J-P Raynauld et al.   ANNALS OF THE RHEUMATIC DISEASES

Prostanoids in health and disease: Fig. 1.

(2008) Emer M. Smyth et al.   JOURNAL OF LIPID RESEARCH

Licofelone Suppresses Prostaglandin E2 Formation by Interference with the Inducible Microsomal Prostaglandin E2 Synthase-1

(2008) A. Koeberle et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS