TY - JOUR
T1 - Class I histone deacetylases catalyze lysine lactylation
AU - Gonzatti, Michelangelo B.
AU - Hintzen, Jordi C.J.
AU - Sharma, Isha
AU - Najar, Mohd Altaf
AU - Tsusaka, Takeshi
AU - Marcinkiewicz, Mariola M.
AU - Da Silva Crispim, Claudia Veronica
AU - Snyder, Nathaniel W.
AU - Burslem, George M.
AU - Goldberg, Emily L.
N1 - Copyright © 2025 The Authors. Published by Elsevier Inc. All rights reserved.
PY - 2025/10
Y1 - 2025/10
N2 - Metabolism and post-translational modifications (PTMs) are intrinsically linked, and the number of identified metabolites that can covalently modify proteins continues to increase. This metabolism/PTM crosstalk is especially true for lactate, the product of anaerobic metabolism following glycolysis. Lactate forms an amide bond with the ε-amino group of lysine, a modification known as lysine lactylation or Kla. Multiple independent mechanisms have been proposed in the formation of Kla, including p300/CBP-dependent transfer from lactyl-CoA, a reactive intermediate lactoylglutathione species that non-enzymatically lactylates proteins, and several enzymes are reported to have lactyl transferase capability. We recently discovered that class I histone deacetylases (HDACs) 1, 2, and 3 can all reverse their canonical chemical reaction to catalyze lysine β-hydroxybutyrylation. Here we tested the hypothesis that HDACs can also catalyze Kla formation. Using biochemical, pharmacological, and genetic approaches, we found that HDACs are sufficient to catalyze Kla formation and that HDACs are a major driver of lysine lactylation. Dialysis experiments confirm this is a reversible reaction that depends on lactate concentration. We also directly quantified intracellular lactyl-CoA and found that Kla abundance can be uncoupled from lactyl-CoA levels. Therefore, we propose a model in which the majority of Kla is formed through enzymatic addition of lactate by HDACs 1, 2, and 3.
AB - Metabolism and post-translational modifications (PTMs) are intrinsically linked, and the number of identified metabolites that can covalently modify proteins continues to increase. This metabolism/PTM crosstalk is especially true for lactate, the product of anaerobic metabolism following glycolysis. Lactate forms an amide bond with the ε-amino group of lysine, a modification known as lysine lactylation or Kla. Multiple independent mechanisms have been proposed in the formation of Kla, including p300/CBP-dependent transfer from lactyl-CoA, a reactive intermediate lactoylglutathione species that non-enzymatically lactylates proteins, and several enzymes are reported to have lactyl transferase capability. We recently discovered that class I histone deacetylases (HDACs) 1, 2, and 3 can all reverse their canonical chemical reaction to catalyze lysine β-hydroxybutyrylation. Here we tested the hypothesis that HDACs can also catalyze Kla formation. Using biochemical, pharmacological, and genetic approaches, we found that HDACs are sufficient to catalyze Kla formation and that HDACs are a major driver of lysine lactylation. Dialysis experiments confirm this is a reversible reaction that depends on lactate concentration. We also directly quantified intracellular lactyl-CoA and found that Kla abundance can be uncoupled from lactyl-CoA levels. Therefore, we propose a model in which the majority of Kla is formed through enzymatic addition of lactate by HDACs 1, 2, and 3.
KW - glycolysis
KW - histone deacetylase (HDAC)
KW - lactate
KW - lactic acid
KW - lysine lactylation
KW - macrophage
KW - post-translational modification (PTM)
KW - protein acylation
UR - https://www.scopus.com/pages/publications/105015368572
U2 - 10.1016/j.jbc.2025.110602
DO - 10.1016/j.jbc.2025.110602
M3 - Article
C2 - 40835008
AN - SCOPUS:105015368572
SN - 0021-9258
VL - 301
SP - 110602
JO - Journal of Biological Chemistry
JF - Journal of Biological Chemistry
IS - 10
M1 - 110602
ER -