Metformin Is a Pyridoxal-5′-phosphate (PLP)-Competitive Inhibitor of SHMT2

Metformin Is a Pyridoxal-5′-phosphate (PLP)-Competitive Inhibitor of SHMT2

The anticancer actions of the biguanide metformin involve the functioning of the serine/glycine one-carbon metabolic network. We report that metformin directly and specifically targets the enzymatic activity of mitochondrial serine hydroxymethyltransferase (SHMT2). In vitro competitive binding assay...

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Bibliographic Details
Main Authors: Angela Tramonti, Elisabet Cuyàs, José Antonio Encinar, Matthias Pietzke, Alessio Paone, Sara Verdura, Aina Arbusà, Begoña Martin-Castillo, Giorgio Giardina, Jorge Joven, Alexei Vazquez, Roberto Contestabile, Francesca Cutruzzolà, Javier A. Menendez
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:Cancers
Subjects:
one-carbon metabolism
serine
glycine
folate
serine hydroxymethyltransferase
Online Access:https://www.mdpi.com/2072-6694/13/16/4009

Internet

https://www.mdpi.com/2072-6694/13/16/4009

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