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Inhibition of the Mitochondrial Carnitine/Acylcarnitine Carrier by Itaconate through Irreversible Binding to Cysteine 136: Possible Pathophysiological Implications.

Nicola GiangregorioAnnamaria TonazziLara ConsoleMariafrancesca ScaliseCesare Indiveri
Published in: Biomolecules (2023)
of mutants in which this Cys was substituted by Val. The central role of C136 was confirmed by covalent docking. Administration of dimethyl itaconate to HeLa cells inhibited the CAC transport activity, suggesting that itaconate could react with the CAC also in intact cells.
Keyphrases
  • induced apoptosis
  • cell cycle arrest
  • oxidative stress
  • endoplasmic reticulum stress
  • signaling pathway
  • pi k akt
  • molecular dynamics simulations
  • small molecule
  • living cells