ArticleEJNMMI research2016
PET imaging of cyclooxygenase-2 (COX-2) in a pre-clinical colorectal cancer model.
Article in EJNMMI research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it, 38 citations in OpenAlex.
- Cyclooxygenase-2 expression is positively associated with lymph node metastasis in nasopharyngeal carcinoma.PloS one · 2017Pooled it
- PET measurement of cyclooxygenase-2 using a novel radioligand: upregulation in primate neuroinflammation and first-in-human study.Journal of neuroinflammation · 2020Trial
- Triarylselenonium triflates provide efficient access to no-carrier-addedChemical science · 2026Article
- A comprehensive review ofMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Radioiodination of Two Carborane-Based Dual Cyclooxygenase-2/5-Lipoxygenase Inhibitors and Their In Vitro and In Vivo Evaluation.Chembiochem : a European journal of chemical biology · 2026Article
- RadiolabeledFrontiers in nuclear medicine · 2025Article
- Radiotracers for Imaging of Inflammatory Biomarkers TSPO and COX-2 in the Brain and in the Periphery.International journal of molecular sciences · 2023Review
- Toward in vivo proof of binding ofEJNMMI research · 2022Article
- Fluorine-18 Labelled Radioligands for PET Imaging of Cyclooxygenase-2.Molecules (Basel, Switzerland) · 2022Review
- Repurposing [Molecular imaging and biology · 2022Article
- Cyclooxygenases as Potential PET Imaging Biomarkers to Explore Neuroinflammation in Dementia.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2022Review
- The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.Journal of medicinal chemistry · 2021Review
- Imaging pheochromocytoma in small animals: preclinical models to improve diagnosis and treatment.EJNMMI research · 2021Review
- Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.ACS medicinal chemistry letters · 2021Article
- Development of PET Radioligands Targeting COX-2 for Colorectal Cancer Staging, a Review ofFrontiers in medicine · 2021Review
- Avicularin Reduces the Expression of Mediators of Inflammation and Oxidative Stress in Bradykinin-Treated MG-63 Human Osteoblastic Osteosarcoma Cells.Medical science monitor : international medical journal of experimental and clinical research · 2020Article
- Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Radiosynthesis and Preclinical Evaluation ofContrast media & molecular imaging · 2019Article
- Evaluation of Two Potent and Selective PET Radioligands to Image COX-1 and COX-2 in Rhesus Monkeys.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2018Article
- 2-(4-Methylsulfonylphenyl)pyrimidines as Prospective Radioligands for Imaging Cyclooxygenase-2 with PET-Synthesis, Triage, and Radiolabeling.Molecules (Basel, Switzerland) · 2018Article
Corrections and comments
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundCyclooxygenase-2 (COX-2) is the inducible isoform of the cyclooxygenase enzyme family. COX-2 is involved in tumor development and progression, and frequent overexpression of COX-2 in a variety of human cancers has made COX-2 an important drug target for cancer treatment. Non-invasive imaging of COX-2 expression in cancer would be useful for assessing COX-2-mediated effects on chemoprevention and radiosensitization using COX-2 inhibitors as an emerging class of anti-cancer drugs, especially for colorectal cancer. Herein, we describe the radiopharmacological analysis of [(18)F]Pyricoxib, a novel radiolabeled COX-2 inhibitor, for specific PET imaging of COX-2 in colorectal cancer.
methodsUptake of [(18)F]Pyricoxib was assessed in human colorectal cancer cell lines HCA-7 (COX-2 positive) and HCT-116 (COX-2 negative). Standard COX-2 inhibitors were used to test for specificity of [(18)F]Pyricoxib for COX-2 binding in vitro and in vivo. PET imaging, biodistribution, and radiometabolite analyses were included into radiopharmacological evaluation of [(18)F]Pyricoxib.
resultsRadiotracer uptake in COX-2 positive HCA-7 cells was significantly higher than in COX-2 negative HCT-116 cells (P < 0.05). COX-2 inhibitors, celecoxib, rofecoxib, and SC58125, blocked uptake of [(18)F]Pyricoxib in HCA-7 cells in a concentration-dependent manner. The radiotracer was slowly metabolized in mice, with approximately 60 % of intact compound after 2 h post-injection. Selective COX-2-mediated tumor uptake of [(18)F]Pyricoxib in HCA-7 xenografts was confirmed in vivo. Celecoxib (100 mg/kg) selectively blocked tumor uptake by 16 % (PET image analysis; P < 0.05) and by 51 % (biodistribution studies; P < 0.01).
conclusionsThe novel PET radiotracer [(18)F]Pyricoxib displays a promising radiopharmacological profile to study COX-2 expression in cancer in vivo.
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