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May 1, 20260 citations

Molecular Basis of α-Glycine C-H Activation by a Nonheme Fe(II)/2-Oxoglutarate Dioxygenase.

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MCManyun ChenTWThisuri N. WanniarachchiJCJonathan D. Caranto

Key Points

  • This research aims to uncover the molecular mechanisms involved in α-glycine C-H activation by nonheme iron enzymes.
  • Utilized kinetic isotope effects and detected transient intermediates in the biochemical reactions.
  • Employed high-resolution crystal structures and molecular dynamics simulations to study the enzyme architecture.
  • Conducted hybrid QM/MM calculations to investigate the reaction mechanisms and energy barriers.
  • Established a low-barrier hydrogen-atom transfer step with significant mechanistic implications.
  • Identified a conserved Trp125 as a crucial part of the electron-transfer network.
  • Revealed structural features that promote substrate positioning in a near-transition-state geometry.

Abstract

performs this unusual chemistry during mycosporine-like amino acid biosynthesis, converting mono- and disubstituted precursors into palythines and revealing unexpected substrate tolerance. Kinetic isotope effects, detection of a transient hydroxylated intermediate, and glyoxylate byproduct formation support an α-hydroxylation-initiated mechanism. High-resolution crystal structures, complemented by molecular docking, molecular dynamics simulations, and site-directed mutagenesis, define an active-site architecture that positions the glycyl substrate in a near-transition-state geometry. Hybrid QM/MM calculations reveal a low-barrier hydrogen-atom-transfer step followed by hydroxyl rebound and implicate a conserved Trp125 in an electron-transfer network that lowers the activation barrier. Together, these findings establish a mechanistic framework for protein-directed α-glycine C-H activation by nonheme iron enzymes and provide a blueprint for engineering Fe/2-OG dioxygenases to expand the chemical diversity of mycosporines and related natural products.

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Cite This Study

Chen et al. (2026) studied this question.

synapsesocial.com/papers/69f44390967e944ac5566bb3https://doi.org/10.1021/acs.biochem.6c00143
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