Structure-based development of small molecule PFKFB3 inhibitors: a framework for potential cancer therapeutic agents targeting the Warburg effect

Cancer cells adopt glycolysis as the major source of metabolic energy production for fast cell growth. The HIF-1-induced PFKFB3 plays a key role in this adaptation by elevating the concentration of Fru-2,6-BP, the most potent glycolysis stimulator. As this metabolic conversion has been suggested to...

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Veröffentlicht in:	PLoS One 2011-09, Vol.6 (9), p.e24179-e24179
Hauptverfasser:	Seo, Minsuh, Kim, Jeong-Do, Neau, David, Sehgal, Inder, Lee, Yong-Hwan
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Apoptosis Benzopyrans - chemistry Benzopyrans - metabolism Benzopyrans - pharmacology Biology Cancer Cell death Cell Death - drug effects Cell Proliferation - drug effects Chemical compounds Chemistry CHEMOTHERAPY Collaboration CRYSTAL STRUCTURE Crystallography Drug Discovery - methods Drug Evaluation, Preclinical DRUGS Energy metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Enzyme kinetics Fructosephosphates - metabolism Gangrene Glucose metabolism GLYCOLYSIS Glycolysis - drug effects Health aspects HeLa Cells Humans Inhibitors Kinases LEAD COMPOUNDS Ligands Medicine Metabolism Models, Molecular Molecular structure NEOPLASMS Pharmacology Phosphofructokinase-2 - antagonists & inhibitors Phosphofructokinase-2 - chemistry Phosphofructokinase-2 - metabolism PRODUCTION Protein Conformation Proteins RESOLUTION Science Studies TARGETS
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