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Gene‐dosage effect of Pfkfb3 on monocyte/macrophage biology in atherosclerosis

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Macrophage‐rich atherosclerotic arteries are highly active in glycolysis. PFKFB3, a key glycolytic enzyme, has emerged as a potential therapeutic target in atherosclerosis. Small‐molecule inhibitors of PFKFB3, such as 3PO and… Click to show full abstract

Macrophage‐rich atherosclerotic arteries are highly active in glycolysis. PFKFB3, a key glycolytic enzyme, has emerged as a potential therapeutic target in atherosclerosis. Small‐molecule inhibitors of PFKFB3, such as 3PO and PFK158, have demonstrated efficacy in hampering atherogenesis in preclinical models. However, genetic studies elucidating the role of Pfkfb3 in atherogenesis need to be conducted to validate pharmacological findings and to unveil potential pharmacological side effects.

Keywords: dosage effect; atherosclerosis; gene dosage; macrophage; biology; pfkfb3

Journal Title: British Journal of Pharmacology
Year Published: 2022

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