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Burer, C.

Publications and source records attributed to Burer, C..

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Evidence for Interaction of 5,10-Methylenetetrahydrofolate Reductase (MTHFR) with Methylenetetrahydrofolate Dehydrogenase (MTHFD1) and General Control Nonderepressible 1 (GCN1)

5,10-methylenetetrahydrofolate reductase (MTHFR) is a folate cycle enzyme required for the intracellular synthesis of methionine. MTHFR was previously shown to be partially phosphorylated at 16 residues, which was abrogated by conversion of threonine 34 to alanine (T34A) or truncation of the first 37 amino acids (i.e. expression of amino acids 38-656), and promoted by methionine supplementation. Here, we over-expressed wild-type MTHFR (MTFHRWT), as well as the variants MTHFRT34A and MTHFR38-656 in 293T cells to provide further insights into these mechanisms. We demonstrate that following incubation in high methionine conditions (100-1000 M) MTHFRWT is almost completely phosphorylated, but in methionine restricted conditions (0-10 M) phosphorylation is reduced, while MTHFRT34A always remains unphosphorylated. Following affinity purification coupled mass spectrometry of an empty vector, MTHFRWT, MTHFRT34A and MTHFR38-656 in three separate experiments, we identified 134 proteins consistently pulled-down by all three MTHFR protein variants, of which 5 were indicated to be likely true interactors (SAINT prediction threshold of 0.95 and 2 fold-change). Amongst these were the folate cycle enzyme methylenetetrahydrofolate dehydrogenase (MTHFD1) and the amino acid starvation sensor General Control Nonderepressible 1 (GCN1). Immunoprecipitation-immunoblotting of MTHFRWT replicated interaction with both proteins. An AlphaFold 3 generated model of the MTHFR-MTHFD1 interaction places the MTHFD1 dehydrogenase/cyclohydrolase domain in direct contact with the MTHFR catalytic domain, suggesting their interaction may facilitate direct delivery of methylenetetrahydrofolate. Overall, we confirm methionine availability increases MTHFR phosphorylation, and identified potential interaction of MTHFR with MTHFD1 and GCN1.

biochemistry↗

Dynamic inter-domain transformations mediate the allosteric regulation of human 5, 10-methylenetetrahydrofolate reductase

5,10-methylenetetrahydrofolate reductase (MTHFR) commits folate-derived one-carbon units to generate the methyl-donor S-adenosyl-L-methionine (SAM). Eukaryotic MTHFR appends to the well-conserved catalytic domain (CD) a unique regulatory domain (RD) that confers feedback inhibition by SAM. We determined cryo-electron microscopy structures of human MTHFR bound to SAM and its demethylated product S-adenosyl-L-homocysteine (SAH). In the active state, with the RD bound to a single SAH, the CD is flexible and exposes its active site for catalysis. However, in the inhibited state the RD pocket is remodelled, exposing a second SAM-binding site that was previously occluded. Dual-SAM bound MTHFR demonstrates a substantially rearranged inter-domain linker that reorients the CD, inserts a loop into the active site, positions Tyr404 to bind the cofactor FAD, and blocks substrate access. Our data therefore explain the long-distance regulatory mechanism of MTHFR inhibition, underpinned by the transition between dual-SAM and single-SAH binding in response to cellular methylation status.

biochemistry↗