AGF347 is a potent inhibitor of serine hydroxymethyltransferase 2 (SHMT2) that inhibits mitochondrial C1 metabolism. It also inhibits cytosolic C1 targets such as SHMT1, GARFTase, and AICARFTase. AGF347 inhibits de novo purine biosynthesis. AGF347 exhibits potent broad spectrum in vitro and in vivo antitumor efficacy.
potent inhibitor of serine hydroxymethyltransferase 2 (SHMT2)
Molecular cancer therapeutics, 18(10), 1787-1799 (2019-07-11)
Folate-dependent one-carbon (C1) metabolism is compartmentalized into the mitochondria and cytosol and supports cell growth through nucleotide and amino acid biosynthesis. Mitochondrial C1 metabolism, including serine hydroxymethyltransferase (SHMT) 2, provides glycine, NAD(P)H, ATP, and C1 units for cytosolic biosynthetic reactions
Folate-dependent one-carbon (C1) metabolism is compartmentalized in the mitochondria and cytosol and is a source of critical metabolites for proliferating tumors. Mitochondrial C1 metabolism including serine hydroxymethyltransferase 2 (SHMT2) generates glycine for de novo purine nucleotide and glutathione biosynthesis and
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