ArticleNature communications2017
In situ click chemistry generation of cyclooxygenase-2 inhibitors.
Article in Nature communications, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 69 papers.
What it found
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Who cites it
69 citing papers in PubMed, 7,514 citations in OpenAlex.
- Shared CD4+ T cell receptor specificity groups in Crohn's disease and ulcerative colitis.JCI insight · 2026Article
- Design, Synthesis, and Evaluation of New Polyhydroxylated Bis-Chalcones as Potential COX-2 Selective Inhibitors.ChemMedChem · 2026Article
- Click Reactions in Kinetic Target-Guided Synthesis: Progress in the Discovery of Inhibitors for Biological Targets.Methods and protocols · 2026Review
- Assembly of CFThe Journal of organic chemistry · 2026Article
- Optimization of galectin-3 binding agents by in situ multiple compound synthesis and native mass spectrometry.Scientific reports · 2026Article
- The complete absence of cytoplasmic γ-actin results in no discernible phenotype in mice or primary fibroblasts.The FEBS journal · 2025Article
- Impact of an oxidative RNA lesion on in vitro replication catalyzed by SARS-CoV-2 RNA-dependent RNA polymerase.The Journal of biological chemistry · 2025Article
- Tumor Diagnosis and Treatment Based on Stimuli-Responsive Aggregation of Gold Nanoparticles.Exploration (Beijing, China) · 2025Review
- Discovery of Boronic Acids-Based β-Lactamase Inhibitors Through In Situ Click Chemistry.International journal of molecular sciences · 2025Article
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- Expanding the Potential Window through Synergistic Design and Oriented Heterostructure for Supercapacitor.Small methods · 2025Article
- Efficient and Rapid Microfluidics Production of Bio-Inspired Nanoparticles Derived fromPharmaceutics · 2025Article
- Enzymatic and microenvironmental regulation in adenosine metabolism-mediated immunosuppression.Frontiers in immunology · 2025Review
- New strategies to enhance the efficiency and precision of drug discovery.Frontiers in pharmacology · 2025Review
- Structure-based protein and small molecule generation using EGNN and diffusion models: A comprehensive review.Computational and structural biotechnology journal · 2024Review
- Biomimetic nanoparticles with red blood cell membranes for enhanced photothermal and immunotherapy for tumors.RSC advances · 2024Article
- Flexible Graphene Field-Effect Transistors and Their Application in Flexible Biomedical Sensing.Nano-micro letters · 2024Review
- Synthesis and elucidation of strained galactopyronose esters as selective cyclooxygenase-2 inhibitor: a comprehensive computational approach.RSC advances · 2024Article
- Review
- Cancer drugs with high repositioning potential for Alzheimer's disease.Expert opinion on emerging drugs · 2023Review
9 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cyclooxygenase-2 isozyme is a promising anti-inflammatory drug target, and overexpression of this enzyme is also associated with several cancers and neurodegenerative diseases. The amino-acid sequence and structural similarity between inducible cyclooxygenase-2 and housekeeping cyclooxygenase-1 isoforms present a significant challenge to design selective cyclooxygenase-2 inhibitors. Herein, we describe the use of the cyclooxygenase-2 active site as a reaction vessel for the in situ generation of its own highly specific inhibitors. Multi-component competitive-binding studies confirmed that the cyclooxygenase-2 isozyme can judiciously select most appropriate chemical building blocks from a pool of chemicals to build its own highly potent inhibitor. Herein, with the use of kinetic target-guided synthesis, also termed as in situ click chemistry, we describe the discovery of two highly potent and selective cyclooxygenase-2 isozyme inhibitors. The in vivo anti-inflammatory activity of these two novel small molecules is significantly higher than that of widely used selective cyclooxygenase-2 inhibitors.Traditional inflammation and pain relief drugs target both cyclooxygenase 1 and 2 (COX-1 and COX-2), causing severe side effects. Here, the authors use in situ click chemistry to develop COX-2 specific inhibitors with high in vivo anti-inflammatory activity.
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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.