ArticleActa pharmacologica Sinica2023
A high-throughput screening campaign against PFKFB3 identified potential inhibitors with novel scaffolds.
Article in Acta pharmacologica Sinica, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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4 citing papers in PubMed, 5 citations in OpenAlex.
- Research progress on the role and therapeutic applications of traditional Chinese medicine in radiation enteropathy.Frontiers in pharmacology · 2026Review
- Innate Immunity Reimagined: Metabolic Reprogramming as a Gateway to Novel Therapeutics.International journal of biological sciences · 2025Review
- High-throughput screen identifies non inflammatory small molecule inducers of trained immunity.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- New Fusarin Derivatives from the Marine Algicolous FungusMarine drugs · 2023Article
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
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Abstract
The growth of solid tumors depends on tumor vascularization and the endothelial cells (ECs) that line the lumen of blood vessels. ECs generate a large fraction of ATP through glycolysis, and elevation of their glycolytic activity is associated with angiogenic behavior in solid tumors. 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) positively regulates glycolysis via fructose-2/6-bisphosphate, the product of its kinase activity. Partial inhibition of glycolysis in tumor ECs by targeting PFKFB3 normalizes the otherwise abnormal tumor vessels, thereby reducing metastasis and improving the outcome of chemotherapy. Although a limited number of tool compounds exist, orally available PFKFB3 inhibitors are unavailable. In this study we conducted a high-throughput screening campaign against the kinase activity of PFKFB3, involving 250,240 chemical compounds. A total of 507 initial hits showing >50% inhibition at 20 µM were identified, 66 of them plus 1 analog from a similarity search consistently displayed low IC
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