A covalent PFKL activator suppresses tumor growth.
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A covalent PFKL activator enhances glycolysis and delivers a CPT2 inhibitor, effectively suppressing tumor growth in vitro and in vivo.
- Why it matters: Targeting cancer's metabolic vulnerabilities, like glycolytic dependency, offers promising therapeutic strategies, but development is hindered by metabolic heterogeneity and resistance.
- What they did: Researchers designed a covalent electrophile-drug conjugate that specifically modifies PFKL at K677, stabilizing its active form and releasing a CPT2 inhibitor to disrupt tumor metabolism.
- The result: This dual-action approach suppresses tumor growth, demonstrating a novel method to target cancer metabolism by combining enzyme activation with targeted delivery of metabolic inhibitors.