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Updated: Jun 5, 2025

Chemiluminescence-based Assays for Detection of Nitric Oxide and its Derivatives from Autoxidation and Nitrosated Compounds
Published on: February 16, 2022
An overview of phenylsulfonylfuroxan-based nitric oxide donors for cancer treatment
Chao Gao1, Xingyu Li1, Tong Liu1
1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China; Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China.
Abstract:
Nitric oxide (NO) is a gaseous molecule integral to numerous physiological processes, including tumor modulation, cardiovascular regulation, and systemic physiological functions. Its dual role in promoting and inhibiting tumor growth makes it a focal point of contemporary oncological research. Phenylsulfonylfuroxan, a classical NO donor, has been shown to significantly elevate NO levels, thereby inducing apoptosis and inhibiting proliferation and metastasis in tumor cells. It enhances the efficacy of chemotherapy, radiotherapy, and immunotherapy, reverses multidrug resistance (MDR), and impedes tumor progression. Notably, phenylsulfonylfuroxan have the ability to trigger ferroptosis in cancer cells by binding covalently to inhibit glutathione peroxidase 4 (GPX4). Recent developments in phenylsulfonylfuroxan-based therapies have positioned them as crucial in the advancement of cancer treatment modalities. This review elucidates the mechanism by which phenylsulfonylfuroxan releases NO and summarizes the significant advancements over the past 16 years in the research and development of phenylsulfonylfuroxan conjugates with various anticancer agents for targeted cancer therapy.
Insights
Phenylsulfonylfuroxan, a nitric oxide (NO) donor, shows promise in cancer therapy by inducing apoptosis and ferroptosis. It enhances existing treatments and combats drug resistance, marking a significant advancement in targeted cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Nitric oxide (NO) plays a complex role in cancer, influencing tumor growth, cardiovascular regulation, and systemic functions.
- Phenylsulfonylfuroxan is a nitric oxide donor that has demonstrated significant potential in modulating tumor behavior.
Purpose of the Study:
- To elucidate the mechanism of nitric oxide release from phenylsulfonylfuroxan.
- To summarize advancements in phenylsulfonylfuroxan conjugates for targeted cancer therapy over the past 16 years.
Main Methods:
- Review of scientific literature focusing on phenylsulfonylfuroxan's mechanism of action and therapeutic applications.
- Analysis of phenylsulfonylfuroxan's role in inducing apoptosis and ferroptosis in cancer cells.
- Examination of phenylsulfonylfuroxan's synergistic effects with chemotherapy, radiotherapy, and immunotherapy.
Main Results:
- Phenylsulfonylfuroxan elevates nitric oxide levels, inducing apoptosis and inhibiting cancer cell proliferation, metastasis, and multidrug resistance (MDR).
- Phenylsulfonylfuroxan triggers ferroptosis by inhibiting glutathione peroxidase 4 (GPX4) in cancer cells.
- Recent developments highlight phenylsulfonylfuroxan conjugates as key components in novel cancer treatment strategies.
Conclusions:
- Phenylsulfonylfuroxan is a versatile agent with significant potential in advancing targeted cancer therapies.
- Its ability to enhance existing treatments and induce specific cancer cell death mechanisms warrants further research and clinical development.
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