Novel leukotriene biosynthesis inhibitors (2012-2016) as anti-inflammatory agents

The 5-lipoxygenase inhibitor RF-22c potently suppresses leukotriene biosynthesis in cellulo and blocks bronchoconstriction and inflammation in vivo

(2016) Anja M. Schaible et al.   BIOCHEMICAL PHARMACOLOGY

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

Development of smart cell-free and cell-based assay systems for investigation of leukotriene C 4 synthase activity and evaluation of inhibitors

(2016) Stefanie Liening et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives

(2016) Pavan Srivastava et al.   BIOORGANIC CHEMISTRY

Structure-activity relationship of caffeic acid phenethyl ester analogs as new 5-lipoxygenase inhibitors

(2016) Jérémie A. Doiron et al.   Chemical Biology & Drug Design

Synthesis and biological evaluation of C(5)-substituted derivatives of leukotriene biosynthesis inhibitor BRP-7

(2016) Serkan Levent et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP)

(2016) Erden Banoglu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Exploring the role of chloro and methyl substitutions in 2-phenylthiomethyl-benzoindole derivatives for 5-LOX enzyme inhibition

(2016) Antonella Peduto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

5-Lipoxygenase-activating protein rescues activity of 5-lipoxygenase mutations that delay nuclear membrane association and disrupt product formation

(2016) Jana Gerstmeier et al.   FASEB JOURNAL

Time-resolved in situ assembly of the leukotriene-synthetic 5-lipoxygenase/5-lipoxygenase-activating protein complex in blood leukocytes

(2016) Jana Gerstmeier et al.   FASEB JOURNAL

Development of novel aminothiazole-comprising 5-LO inhibitors

(2016) Simon B M Kretschmer et al.   Future Medicinal Chemistry

Phosphorylation of Leukotriene C4Synthase at Serine 36 Impairs Catalytic Activity

(2016) Shabbir Ahmad et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis of [3H] and [2H6]AZD6642, an inhibitor of 5-lipoxygenase activating protein (FLAP)

(2016) Åsa Lindelöf et al.   JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions

(2016) Andreas Koeberle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase

(2016) Yu Zhou et al.   Acta Pharmaceutica Sinica B

A phase 2 randomized, double-blind, placebo-controlled study of the effect of VIA-2291, a 5-lipoxygenase inhibitor, on vascular inflammation in patients after an acute coronary syndrome

(2015) Juan Gaztanaga et al.   ATHEROSCLEROSIS

Transcellular biosynthesis of eicosanoid lipid mediators

(2015) Valérie Capra et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Biosynthesis, biological effects, and receptors of hydroxyeicosatetraenoic acids (HETEs) and oxoeicosatetraenoic acids (oxo-ETEs) derived from arachidonic acid

(2015) William S. Powell et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

5-Lipoxygenase, a key enzyme for leukotriene biosynthesis in health and disease

(2015) Olof Rådmark et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS

Recent advances for FLAP inhibitors

(2015) Daniel Pettersen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Harnessing Enzymatic Promiscuity in Myxochelin Biosynthesis for the Production of 5-Lipoxygenase Inhibitors

(2015) Juliane Korp et al.   CHEMBIOCHEM

Synthesis and Biological Evaluation of N-Aryl-5-aryloxazol-2-amine Derivatives as 5-Lipoxygenase Inhibitors

(2015) Jee Hee Suh et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Development and evaluation of ST-1829 based on 5-benzylidene-2-phenylthiazolones as promising agent for anti-leukotriene therapy

(2015) Andreas P. Lill et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel series of benzoquinones with high potency against 5-lipoxygenase in human polymorphonuclear leukocytes

(2015) Rosanna Filosa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors

(2015) Daniela De Lucia et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Lipoxin and resolvin biosynthesis is dependent on 5-lipoxygenase activating protein

(2015) Christoph Lehmann et al.   FASEB JOURNAL

Synthesis, SAR, and Series Evolution of Novel Oxadiazole-Containing 5-Lipoxygenase Activating Protein Inhibitors: Discovery of 2-[4-(3-{(R)-1-[4-(2-Amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915)

(2015) Hidenori Takahashi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Myxochelins Target Human 5-Lipoxygenase

(2015) Sebastian Schieferdecker et al.   JOURNAL OF NATURAL PRODUCTS

Development of an Asymmetric Synthesis of a Chiral Quaternary FLAP Inhibitor

(2015) Keith R. Fandrick et al.   JOURNAL OF ORGANIC CHEMISTRY

Neutrophils support lung colonization of metastasis-initiating breast cancer cells

(2015) Stefanie K. Wculek et al.   NATURE

The effect of GSK2190915, a 5-lipoxygenase‐activating protein inhibitor, on exercise-induced bronchoconstriction

(2014) Sandra E . Kent et al.   ALLERGY AND ASTHMA PROCEEDINGS

An experimental cell-based model for studying the cell biology and molecular pharmacology of 5-lipoxygenase-activating protein in leukotriene biosynthesis

(2014) Jana Gerstmeier et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

The novel benzimidazole derivative BRP-7 inhibits leukotriene biosynthesisin vitroandin vivoby targeting 5-lipoxygenase-activating protein (FLAP)

(2014) C Pergola et al.   BRITISH JOURNAL OF PHARMACOLOGY

Elucidation of the molecular mechanism and the efficacyin vivoof a novel 1,4-benzoquinone that inhibits 5-lipoxygenase

(2014) A M Schaible et al.   BRITISH JOURNAL OF PHARMACOLOGY

Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7

(2014) Magnus Bäck et al.   BRITISH JOURNAL OF PHARMACOLOGY

Further studies on ethyl 5-hydroxy-indole-3-carboxylate scaffold: Design, synthesis and evaluation of 2-phenylthiomethyl-indole derivatives as efficient inhibitors of human 5-lipoxygenase

(2014) Antonella Peduto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Targeting 5-lipoxygenase-activating protein in asthma and chronic obstructive pulmonary disease

(2014) Sabina Antonela Antoniu   EXPERT OPINION ON THERAPEUTIC TARGETS

Discovery of AZD6642, an Inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the Treatment of Inflammatory Diseases

(2014) Malin Lemurell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Indirubin Core Structure of Glycogen Synthase Kinase-3 Inhibitors as Novel Chemotype for Intervention with 5-Lipoxygenase

(2014) Carlo Pergola et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pro-resolving lipid mediators are leads for resolution physiology

(2014) Charles N. Serhan   NATURE

Exploring the roles of UGT1A1 and UGT1A3 in oral clearance of GSK2190915, a 5-lipoxygenase-activating protein inhibitor

(2014) Michael Mosteller et al.   Pharmacogenetics and Genomics

Roles of coactosin-like protein (CLP) and 5-lipoxygenase-activating protein (FLAP) in cellular leukotriene biosynthesis

(2014) D. Basavarajappa et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Binding of Pro-Gly-Pro at the active site of leukotriene A4 hydrolase/aminopeptidase and development of an epoxide hydrolase selective inhibitor

(2014) A. Stsiapanava et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of JNJ-40929837, a leukotriene A4 hydrolase inhibitor, in a bronchial allergen challenge model of asthma

(2014) W. Barchuk et al.   PULMONARY PHARMACOLOGY & THERAPEUTICS

Testicular distribution and toxicity of a novel LTA4H inhibitor in rats

(2014) P.D. Ward et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

Inhibitors of the Arachidonic Acid Cascade: Interfering with Multiple Pathways

(2013) Karin Meirer et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Recent Advances in the Search for Novel 5-Lipoxygenase Inhibitors

(2013) Dieter Steinhilber et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Potent inhibition of human 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 by the anti-carcinogenic and anti-inflammatory agent embelin

(2013) Anja M. Schaible et al.   BIOCHEMICAL PHARMACOLOGY

Discovery and biological evaluation of novel 1,4-benzoquinone and related resorcinol derivatives that inhibit 5-lipoxygenase

(2013) Rosanna Filosa et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure–activity relationship and in vitro pharmacological evaluation of imidazo[1,2-a]pyridine-based inhibitors of 5-LO

(2013) Estel.la Buscató et al.   Future Medicinal Chemistry

A leukotriene C4 synthase inhibitor with the backbone of 5-(5-methylene-4-oxo-4,5-dihydrothiazol-2-ylamino) isophthalic acid

(2013) Hideo Ago et al.   JOURNAL OF BIOCHEMISTRY

Aminothiazole-Featured Pirinixic Acid Derivatives As Dual 5-Lipoxygenase and Microsomal Prostaglandin E2 Synthase-1 Inhibitors with Improved Potency and Efficiency in Vivo

(2013) Thomas Hanke et al.   JOURNAL OF MEDICINAL CHEMISTRY

Neutrophil swarms require LTB4 and integrins at sites of cell death in vivo

(2013) Tim Lämmermann et al.   NATURE

Efficacy, safety and tolerability of GSK2190915, a 5-lipoxygenase activating protein inhibitor, in adults and adolescents with persistent asthma: a randomised dose-ranging study

(2013) Richard MA Follows et al.   RESPIRATORY RESEARCH

Synthesis and biological evaluation of a class of 5-benzylidene-2-phenyl-thiazolinones as potent 5-lipoxygenase inhibitors

(2012) Sebastian Barzen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP)

(2012) Erden Banoglu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Azabenzthiazole inhibitors of leukotriene A4 hydrolase

(2012) Virginia M. Tanis et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

SAR-study on a new class of imidazo[1,2-a]pyridine-based inhibitors of 5-lipoxygenase

(2012) Martina Hieke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification of benzofuran central cores for the inhibition of leukotriene A4 hydrolase

(2012) Wendy Eccles et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor

(2012) Gretchen Bain et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Cysteinyl leukotriene receptors, old and new; implications for asthma

(2012) T. M. Laidlaw et al.   CLINICAL AND EXPERIMENTAL ALLERGY

Optimization of 5-hydroxytryptamines as dual function inhibitors targeting phospholipase A2 and leukotriene A4 hydrolase

(2012) Hu Meng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Overview of recent drug discovery approaches for new generation leukotriene A4 hydrolase inhibitors

(2012) Burcu Çalışkan et al.   Expert Opinion on Drug Discovery

The nuclear membrane leukotriene synthetic complex is a signal integrator and transducer

(2012) Angela M. Bair et al.   MOLECULAR BIOLOGY OF THE CELL

Molecular characterization of EP6—A novel imidazo[1,2-a]pyridine based direct 5-lipoxygenase inhibitor

(2011) Joanna M. Wisniewska et al.   BIOCHEMICAL PHARMACOLOGY

Lipoxygenase and Leukotriene Pathways: Biochemistry, Biology, and Roles in Disease

(2011) Jesper Z. Haeggström et al.   CHEMICAL REVIEWS

Testosterone suppresses phospholipase D, causing sex differences in leukotriene biosynthesis in human monocytes

(2011) Carlo Pergola et al.   FASEB JOURNAL

The Catalytic Architecture of Leukotriene C4Synthase with Two Arginine Residues

(2011) Hiromichi Saino et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Regulation of inflammation in cancer by eicosanoids

(2011) Emily R. Greene et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

The Structure of Human 5-Lipoxygenase

(2011) N. C. Gilbert et al.   SCIENCE

5-Lipoxygenase inhibitors: a review of recent developments and patents

(2010) Carlo Pergola et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Location, Location, Location: Compartmentalization of Early Events in Leukotriene Biosynthesis

(2010) Marcia E. Newcomer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Critical Role for LTA4H in Limiting Chronic Pulmonary Neutrophilic Inflammation

(2010) R. J. Snelgrove et al.   SCIENCE

Distinct parts of leukotriene C4 synthase interact with 5-lipoxygenase and 5-lipoxygenase activating protein

(2009) Tobias Strid et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Sulindac sulfide suppresses 5-lipoxygenase at clinically relevant concentrations

(2009) Svenja D. Steinbrink et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Hyperforin is a novel type of 5-lipoxygenase inhibitor with high efficacy in vivo

(2009) Christian Feißt et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Structural Optimization and Biological Evaluation of 2-Substituted 5-Hydroxyindole-3-carboxylates as Potent Inhibitors of Human 5-Lipoxygenase

(2009) Eva-Maria Karg et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4-[(2S)-2-{[4-(4-Chlorophenoxy)phenoxy]methyl}-1-pyrrolidinyl]butanoic Acid (DG-051) as a Novel Leukotriene A4 Hydrolase Inhibitor of Leukotriene B4 Biosynthesis

(2009) Vincent Sandanayaka et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phosphorylation of Serine 271 on 5-Lipoxygenase and Its Role in Nuclear Export

(2008) Nicolas Flamand et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The nuclear membrane organization of leukotriene synthesis

(2008) A. K. Mandal et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

ERK-mediated regulation of leukotriene biosynthesis by androgens: A molecular basis for gender differences in inflammation and asthma

(2008) C. Pergola et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

What's all the FLAP about?: 5-lipoxygenase-activating protein inhibitors for inflammatory diseases

(2008) J EVANS et al.   TRENDS IN PHARMACOLOGICAL SCIENCES