ArticleScientific reports2018
Structure-based discovery of mPGES-1 inhibitors suitable for preclinical testing in wild-type mice as a new generation of anti-inflammatory drugs.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 41 citations in OpenAlex.
- Prenylated apigenin derivatives from Cannabis sativa L.: isolation, biosynthesis, and anti-inflammatory properties.Journal of cannabis research · 2026Article
- 5-methyl-2-carboxamidepyrrole-based novel dual mPGES-1/sEH inhibitors as promising anticancer candidates.Archiv der Pharmazie · 2025Article
- A highly selective mPGES-1 inhibitor to block abdominal aortic aneurysm progression in the angiotensin mouse model.Scientific reports · 2024Article
- Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity.Molecular diversity · 2023Article
- Design, synthesis and characterization of lead compounds as anti-inflammatory drugs targeting mPGES-1 via enzymelink screening.Future medicinal chemistry · 2023Article
- Analgesic effects of a highly selective mPGES-1 inhibitor.Scientific reports · 2023Article
- Identification of 2-Aminoacyl-1,3,4-thiadiazoles as Prostaglandin EACS medicinal chemistry letters · 2023Article
- Development of pharmacotherapies for abdominal aortic aneurysms.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2022Review
- Latest progress in the development of cyclooxygenase-2 pathway inhibitors targeting microsomal prostaglandin EFuture medicinal chemistry · 2022Article
- Aurantiamide Acetate Ameliorates Lung Inflammation in Lipopolysaccharide-Induced Acute Lung Injury in Mice.BioMed research international · 2022Article
- Engineering 'Enzymelink' for screening lead compounds to inhibit mPGES-1 while maintaining prostacyclin synthase activity.Future medicinal chemistry · 2021Article
- Orally Administered NSAIDs-General Characteristics and Usage in the Treatment of Temporomandibular Joint Osteoarthritis-A Narrative Review.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Overview on the Discovery and Development of Anti-Inflammatory Drugs: Should the Focus Be on Synthesis or Degradation of PGEJournal of inflammation research · 2021Review
- Identification of 2-(thiophen-2-yl)acetic Acid-Based Lead Compound for mPGES-1 Inhibition.Frontiers in chemistry · 2021Article
- Targeting microsomal prostaglandin E synthase 1 to develop drugs treating the inflammatory diseases.American journal of translational research · 2021Article
- DREAM-in-CDM Approach and Identification of a New Generation of Anti-inflammatory Drugs Targeting mPGES-1.Scientific reports · 2020Article
- Discovery and Development of a Novel mPGES-1/5-LOX Dual Inhibitor LFA-9 for Prevention and Treatment of Chronic Inflammatory Diseases.Journal of inflammation research · 2020Article
- Biological characterization of new inhibitors of microsomal PGE synthase-1 in preclinical models of inflammation and vascular tone.British journal of pharmacology · 2019Article
- Long-Lasting Anti-Inflammatory and Antinociceptive Effects of Acute Ammonium Glycyrrhizinate Administration: Pharmacological, Biochemical, and Docking Studies.Molecules (Basel, Switzerland) · 2019Article
- The COX2 Effector Microsomal PGE2 Synthase 1 is a Regulator of Immunosuppression in Cutaneous Melanoma.Clinical cancer research : an official journal of the American Association for Cancer Research · 2019Article
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10 authors at 1 institution in 1 country.
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Abstract
Human mPGES-1 is recognized as a promising target for next generation of anti-inflammatory drugs without the side effects of currently available anti-inflammatory drugs, and various inhibitors have been reported in the literature. However, none of the reported potent inhibitors of human mPGES-1 has shown to be also a potent inhibitor of mouse or rat mPGES-1, which prevents using the well-established mouse/rat models of inflammation-related diseases for preclinical studies. Hence, despite of extensive efforts to design and discover various human mPGES-1 inhibitors, the promise of mPGES-1 as a target for the next generation of anti-inflammatory drugs has never been demonstrated in any wild-type mouse/rat model using an mPGES-1 inhibitor. Here we report discovery of a novel type of selective mPGES-1 inhibitors potent for both human and mouse mPGES-1 enzymes through structure-based rational design. Based on in vivo studies using wild-type mice, the lead compound is indeed non-toxic, orally bioavailable, and more potent in decreasing the PGE
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