A pyrazolopyran derivative preferentially inhibits the activity of human cytosolic serine hydroxymethyltransferase and induces cell death in lung cancer cells

Serine hydroxymethyltransferase (SHMT) is a central enzyme in the metabolic reprogramming of cancer cells, providing activated one-carbon units in the serine-glycine one-carbon metabolism. Previous studies demonstrated that the cytoplasmic isoform of SHMT (SHMT1) plays a relevant role in lung cancer...

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Veröffentlicht in:	Oncotarget 2016-01, Vol.7 (4), p.4570-4583
Hauptverfasser:	Marani, Marina, Paone, Alessio, Fiascarelli, Alessio, Macone, Alberto, Gargano, Maurizio, Rinaldo, Serena, Giardina, Giorgio, Pontecorvi, Valentino, Koes, David, McDermott, Lee, Yang, Tianyi, Paiardini, Alessandro, Contestabile, Roberto, Cutruzzolà, Francesca
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - pharmacology Apoptosis - drug effects Blotting, Western Catalytic Domain Cell Proliferation - drug effects Cytoplasm - enzymology Enzyme Inhibitors - pharmacology Glycine Hydroxymethyltransferase - chemistry Glycine Hydroxymethyltransferase - genetics Glycine Hydroxymethyltransferase - metabolism Humans Immunoenzyme Techniques Lung Neoplasms - drug therapy Lung Neoplasms - genetics Lung Neoplasms - metabolism Lung Neoplasms - pathology Molecular Dynamics Simulation Protein Conformation Pyrans - chemistry Pyrazoles - chemistry Real-Time Polymerase Chain Reaction Research Paper Reverse Transcriptase Polymerase Chain Reaction RNA, Messenger - genetics Tumor Cells, Cultured
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