Identification and development of mPGES-1 inhibitors: where we are at?

Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1

(2011) Christine Greiner et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Trisubstituted ureas as potent and selective mPGES-1 inhibitors

(2011) Jean-François Chiasson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A novel class of dual mPGES-1/5-LO inhibitors based on the α-naphthyl pirinixic acid scaffold

(2011) Martina Hieke et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-Based Discovery of Inhibitors of Microsomal Prostaglandin E2Synthase−1, 5-Lipoxygenase and 5-Lipoxygenase-Activating Protein: Promising Hits for the Development of New Anti-inflammatory Agents

(2011) Rosa De Simone et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pharmacophore Modeling and Virtual Screening for Novel Acidic Inhibitors of Microsomal Prostaglandin E2Synthase-1 (mPGES-1)

(2011) Birgit Waltenberger et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hyperforin, an Anti-Inflammatory Constituent from St. John's Wort, Inhibits Microsomal Prostaglandin E2 Synthase-1 and Suppresses Prostaglandin E2 Formation in vivo

(2011) Andreas Koeberle et al.   Frontiers in Pharmacology

Expression of cyclooxygenase-2 and microsomal prostagalandin E synthase-1 in head and neck squamous cell carcinoma

(2010) Ryo Kawata et al.   AURIS NASUS LARYNX

Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor

(2010) Gabriel Mbalaviele et al.   BIOCHEMICAL PHARMACOLOGY

Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo

(2010) Julia Bauer et al.   BIOCHEMICAL PHARMACOLOGY

mPGES-1 as a target for cancer suppression

(2010) Masako Nakanishi et al.   BIOCHIMIE

Prostaglandin E synthases: Understanding their pathophysiological roles through mouse genetic models

(2010) Shuntaro Hara et al.   BIOCHIMIE

Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

(2010) Tom Y.H. Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Selective inducible microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitors derived from an oxicam template

(2010) Jane Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of microsomal prostaglandin E2 synthase-1 as a molecular basis for the anti-inflammatory actions of boswellic acids from frankincense

(2010) U Siemoneit et al.   BRITISH JOURNAL OF PHARMACOLOGY

Identification of Key Residues Determining Species Differences in Inhibitor Binding of Microsomal Prostaglandin E Synthase-1

(2010) Sven-Christian Pawelzik et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Understanding Microscopic Binding of Human Microsomal Prostaglandin E Synthase-1 (mPGES-1) Trimer with Substrate PGH2and Cofactor GSH: Insights from Computational Alanine Scanning and Site-directed Mutagenesis

(2010) Adel Hamza et al.   JOURNAL OF PHYSICAL CHEMISTRY B

Co-Overexpression of Cyclooxygenase-2 and Microsomal Prostaglandin E Synthase-1 Adversely Affects the Postoperative Survival in Non-small Cell Lung Cancer

(2010) Yu-Chung Wu et al.   Journal of Thoracic Oncology

mPGES-1 expression in non-cancerous liver tissue impacts on postoperative recurrence of HCC

(2010) Koichi Nonaka   WORLD JOURNAL OF GASTROENTEROLOGY

Impacts of Cytosolic Phospholipase A2, 15-Prostaglandin Dehydrogenase, and Cyclooxygenase-2 Expressions on Tumor Progression in Colorectal Cancer

(2010) Sung Chul Lim et al.   YONSEI MEDICAL JOURNAL

Immunohistochemical Demonstration of Membrane-bound Prostaglandin E2 Synthase-1 in Papillary Thyroid Carcinoma

(2009) Yoko Omi et al.   ACTA HISTOCHEMICA ET CYTOCHEMICA

Green tea epigallocatechin-3-gallate inhibits microsomal prostaglandin E 2 synthase-1

(2009) Andreas Koeberle et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Microsomal prostaglandin E synthase-1 in both cancer cells and hosts contributes to tumour growth, invasion and metastasis

(2009) Daisuke Kamei et al.   BIOCHEMICAL JOURNAL

Identification of 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 as functional targets of the anti-inflammatory and anti-carcinogenic garcinol

(2009) Andreas Koeberle et al.   BIOCHEMICAL PHARMACOLOGY

Effects of AF3442 [ N -(9-ethyl-9 H -carbazol-3-yl)-2-(trifluoromethyl)benzamide], a novel inhibitor of human microsomal prostaglandin E synthase-1, on prostanoid biosynthesis in human monocytes in vitro

(2009) Annalisa Bruno et al.   BIOCHEMICAL PHARMACOLOGY

Discovery of benzo[g]indol-3-carboxylates as potent inhibitors of microsomal prostaglandin E2 synthase-1

(2009) Andreas Koeberle et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors

(2009) André Giroux et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Myrtucommulone, a natural acylphloroglucinol, inhibits microsomal prostaglandin E2 synthase-1

(2009) A Koeberle et al.   BRITISH JOURNAL OF PHARMACOLOGY

Arylpyrrolizines as Inhibitors of Microsomal Prostaglandin E2Synthase-1 (mPGES-1) or as Dual Inhibitors of mPGES-1 and 5-Lipoxygenase (5-LOX)

(2009) Andy J. Liedtke et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Nonacidic Inhibitors of Human Microsomal Prostaglandin Synthase 1 (mPGES 1) Identified by a Multistep Virtual Screening Protocol

(2009) Florian Rörsch et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Practical Synthesis ofm-Prostaglandin E Synthase-1 Inhibitor MK-7285

(2009) Francis Gosselin et al.   JOURNAL OF ORGANIC CHEMISTRY

The Molecular Pharmacology and In Vivo Activity of 2-(4-Chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a Dual Inhibitor of Microsomal Prostaglandin E2 Synthase-1 and 5-Lipoxygenase

(2009) A. Koeberle et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Curcumin blocks prostaglandin E2 biosynthesis through direct inhibition of the microsomal prostaglandin E2 synthase-1

(2009) A. Koeberle et al.   MOLECULAR CANCER THERAPEUTICS

Expression Analysis of the Prostaglandin E2 Production Pathway in Human Pancreatic Cancers

(2009) Sascha Hasan et al.   PANCREAS

Microsomal prostaglandin E synthase 1 determines tumor growth in vivo of prostate and lung cancer cells

(2009) H. Hanaka et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Comparison of microsomal prostaglandin E synthase-1 deletion and COX-2 inhibition in acute cardiac ischemia in mice

(2009) Dongmei Wu et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

The effects of microsomal prostaglandin E synthase-1 deletion in acute cardiac ischemia in mice

(2009) Dongmei Wu et al.   PROSTAGLANDINS LEUKOTRIENES AND ESSENTIAL FATTY ACIDS

Photo-crosslinking of proteins in intact cells reveals a dimeric structure of cyclooxygenase-2 and an inhibitor-sensitive oligomeric structure of microsomal prostaglandin E2 synthase-1

(2008) Pierre-Olivier Hétu et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Dimethylcelecoxib inhibits prostaglandin E2 production

(2008) Ivonne Wobst et al.   BIOCHEMICAL PHARMACOLOGY

High expression of PGE2 enzymatic pathways in cervical (pre)neoplastic lesions and functional consequences for antigen-presenting cells

(2008) Michaël Herfs et al.   CANCER IMMUNOLOGY IMMUNOTHERAPY

Genetic Deletion of mPGES-1 Suppresses Intestinal Tumorigenesis

(2008) M. Nakanishi et al.   CANCER RESEARCH

Microsomal Prostaglandin E 2 Synthase-1 Deletion Leads to Adverse Left Ventricular Remodeling After Myocardial Infarction

(2008) Norbert Degousee et al.   CIRCULATION

COX-2 gene polymorphisms and protein expression in renomedullary interstitial cell tumors

(2008) Zoran Gatalica et al.   HUMAN PATHOLOGY

Mutation of a Critical Arginine in Microsomal Prostaglandin E Synthase-1 Shifts the Isomerase Activity to a Reductase Activity That Converts Prostaglandin H2into Prostaglandin F2α

(2008) Tove Hammarberg et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Homo-timeric structural model of human microsomal prostaglandin E synthase-1 and characterization of its substrate/inhibitor binding interactions

(2008) Li Xing et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Novel and Potent Inhibitors of 5-Lipoxygenase Product Synthesis Based on the Structure of Pirinixic Acid

(2008) Oliver Werz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pirinixic Acid Derivatives as Novel Dual Inhibitors of Microsomal Prostaglandin E2Synthase-1 and 5-Lipoxygenase

(2008) Andreas Koeberle et al.   JOURNAL OF MEDICINAL CHEMISTRY

MF63 [2-(6-Chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a Selective Microsomal Prostaglandin E Synthase-1 Inhibitor, Relieves Pyresis and Pain in Preclinical Models of Inflammation

(2008) D. Xu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

Tumor-growth–promoting cyclooxygenase-2 prostaglandin E2 pathway provides medulloblastoma therapeutic targets

(2008) Ninib Baryawno et al.   NEURO-ONCOLOGY

The terminal prostaglandin synthases mPGES-1, mPGES-2, and cPGES are all overexpressed in human gliomas

(2008) Simo Mattila et al.   NEUROPATHOLOGY

Structural basis for induced formation of the inflammatory mediator prostaglandin E2

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

Microsomal prostaglandin E synthase-2 is not essential for in vivo prostaglandin E2 biosynthesis

(2008) Leigh A. Jania et al.   PROSTAGLANDINS & OTHER LIPID MEDIATORS

Expression of prostaglandin E synthase in Barrett’s cancer

(2007) B. H. A. von Rahden et al.   DISEASES OF THE ESOPHAGUS