ArticleNature chemical biology2011
(R)-Profens are substrate-selective inhibitors of endocannabinoid oxygenation by COX-2.
Article in Nature chemical biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 80 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
80 citing papers in PubMed, 180 citations in OpenAlex.
- Intrathecal morphine administration reduces postoperative pain and peripheral endocannabinoid levels in total knee arthroplasty patients: a randomized clinical trial.BMC anesthesiology · 2018Trial
- Substrate-Selective Inhibition of the SARS-CoV-2 Papain-Like Protease: Inhibition of Hydrolysis of Human Over Viral Substrates.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Identification of Clofibric Acid as a Synoviolin (SYVN1) Ligand for Proteolysis-Targeting Chimera (PROTAC) Development.ACS medicinal chemistry letters · 2026Article
- Metabolites extracted from browntop millet (Urochloa ramosa (L.) T.Q. Nguyen) mitigated the proliferation of breast- and colorectal carcinoma cellsFrontiers in pharmacology · 2026Article
- Substrate-selective COX-2 inhibition by IMMA attenuates posttraumatic headache via endocannabinoid modulation and neuroinflammatory suppression.The journal of headache and pain · 2025Article
- In vivo anti-inflammatory evaluation of oxadiazole derivatives bearing flurbiprofen moiety using experimental and computational approaches.Scientific reports · 2025Article
- Chemical inhibition of Arabidopsis PIN-FORMED auxin transporters by the anti-inflammatory drug naproxen.Plant communications · 2023Article
- Article
- Phytochemical profile, comparative evaluation of Satureja montana alcoholic extract for antioxidants, anti-inflammatory and molecular docking studies.BMC complementary medicine and therapies · 2023Article
- Inhibiting degradation of 2-arachidonoylglycerol as a therapeutic strategy for neurodegenerative diseases.Pharmacology & therapeutics · 2023Review
- Substrate-selective small-molecule modulators of enzymes: Mechanisms and opportunities.Current opinion in chemical biology · 2023Review
- Effect of Post-Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides.Antibiotics (Basel, Switzerland) · 2023Review
- 2-Arylpropionic Acid Pyrazolamides as Cannabinoid CB2 Receptor Inverse Agonists Endowed with Anti-Inflammatory Properties.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Assessment of NSAIDs as potential inhibitors of the fatty acid amide hydrolase I (FAAH-1) using three different primary fatty acid amide substrates in vitro.BMC pharmacology & toxicology · 2022Article
- The Search for Cyclooxygenase-2 (COX-2) Inhibitors for the Treatment of Inflammation Disease: An in-silico Study.Journal of multidisciplinary healthcare · 2022Article
- Fungicidal amphotericin B sponges are assemblies of staggered asymmetric homodimers encasing large void volumes.Nature structural & molecular biology · 2021Article
- Design, synthesis andJournal of enzyme inhibition and medicinal chemistry · 2021Article
- Limitations of drug concentrations used in cell culture studies for understanding clinical responses of NSAIDs.Inflammopharmacology · 2021Review
- Article
- The endocannabinoid system - current implications for drug development.Journal of internal medicine · 2021Review
20 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
Cyclooxygenase-2 (COX-2) catalyzes the oxygenation of arachidonic acid and the endocannabinoids 2-arachidonoylglycerol and arachidonoylethanolamide. Evaluation of a series of COX-2 inhibitors revealed that many weak competitive inhibitors of arachidonic acid oxygenation are potent inhibitors of endocannabinoid oxygenation. (R) enantiomers of ibuprofen, naproxen and flurbiprofen, which are considered to be inactive as COX-2 inhibitors, are potent 'substrate-selective inhibitors' of endocannabinoid oxygenation. Crystal structures of the COX-2–(R)-naproxen and COX-2–(R)-flurbiprofen complexes verified this unexpected binding and defined the orientation of the (R) enantiomers relative to (S) enantiomers. (R)-Profens selectively inhibited endocannabinoid oxygenation by lipopolysaccharide-stimulated dorsal root ganglion (DRG) cells. Substrate-selective inhibition provides new tools for investigating the role of COX-2 in endocannabinoid oxygenation and a possible explanation for the ability of (R)-profens to maintain endocannabinoid tone in models of neuropathic pain.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.