At Ace Therapeutics, we specialize in the development of cyclooxygenase-2 (COX-2) inhibitors. With a deep understanding of the critical role COX-2 plays in inflammation and disease progression, our team of experts is dedicated to tailoring drug development solutions to address diseases such as colorectal cancer, inflammatory bowel disease, and liver cirrhosis.
The Role of COX-2 in Gastroenterology and Hepatology
COX-2 is significantly upregulated and contributes to the pathogenesis of gastrointestinal and liver diseases such as colorectal cancer, inflammatory bowel disease, and liver cirrhosis. Its overexpression is associated with increased inflammation, cellular proliferation, and resistance to apoptosis, all of which can exacerbate disease progression. Selective COX-2 inhibitors have the potential to mitigate inflammation and tumorigenesis while minimizing the gastrointestinal side effects associated with non-selective COX inhibitors, thus offering a targeted therapeutic strategy for managing gastrointestinal and liver diseases.
Figure 1. Potential mechanisms of COX-2 in the process of liver fibrosis. (Yang H., et al., 2020)
What Can We Do for the Development of COX-2 Inhibitors?
At Ace Therapeutics, we have extensive experience assisting our customers in validating the critical role of COX-2 in the pathogenesis of different gastrointestinal and liver diseases, exploring its potential as a promising drug target.
We can help you identify and optimize potential COX-2 inhibitor candidates using advanced screening technologies and medicinal chemistry expertise.
- Evaluation of Drug Efficacy
In Vitro Evaluation
In Vivo Evaluation
- Enzyme Assays: Perform enzyme assays to determine the potency and selectivity of COX-2 inhibitors against COX-1 and other relevant enzymes.
- Cell Viability Assays: Test the effect of COX-2 inhibitors on the viability of gastrointestinal and liver cell lines.
- Prostaglandin Assays: Measure the inhibition of prostaglandin synthesis to evaluate the efficacy of COX-2 inhibition.
- Anti-inflammatory Assays: Evaluate the reduction of inflammatory markers such as IL-6, TNF-α, and COX-2 expression in drug treated cells.
- Apoptosis Assays: Assess the induction of apoptosis in cancer cell lines to determine potential anti-tumor effects.
- Inflammatory Bowel Disease (IBD) Models: Employe animal models such as DSS-induced colitis or TNBS-induced colitis to test the anti-inflammatory effects of COX-2 inhibitors.
- Liver Fibrosis Models & Liver Cirrhosis Models: Utilize carbon tetrachloride (CCl4)-induced or bile duct ligation (BDL) models to investigate the protective effects of COX-2 inhibitors on liver fibrosis and inflammation.
- Animal Models of Colorectal Cancer: Use chemically induced models (e.g., azoxymethane (AOM) and dextran sulfate sodium (DSS)) to evaluate the efficacy of COX-2 inhibitors in reducing tumor formation and progression.
- Genetically Engineered Mouse Models: Custom mice with specific genetic modifications to study the role of COX-2 inhibition in various gastrointestinal and liver diseases.
From target identification and lead optimization to preclinical studies, Ace Therapeutics offers a full spectrum of services to support your COX-2 inhibitor development project. Contact us to harness the potential of COX-2 inhibition and improve drug therapy for gastrointestinal and liver diseases.
References
- Yang H., et al. COX-2 in liver fibrosis. Clin Chim Acta. 2020, 506:196-203.
- Wang D., Dubois R.N. The role of COX-2 in intestinal inflammation and colorectal cancer. Oncogene. 2010, 29(6):781-8.
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