Lipoylation inhibition enhances radiation control of lung cancer by suppressing homologous recombination DNA damage repair

Sci Adv. 2025 Mar 14;11(11):eadt1241. doi: 10.1126/sciadv.adt1241. Epub 2025 Mar 12.

Abstract

Lung cancer exhibits altered metabolism, influencing its response to radiation. To investigate the metabolic regulation of radiation response, we conducted a comprehensive, metabolic-wide CRISPR-Cas9 loss-of-function screen using radiation as selection pressure in human non-small cell lung cancer. Lipoylation emerged as a key metabolic target for radiosensitization, with lipoyltransferase 1 (LIPT1) identified as a top hit. LIPT1 covalently conjugates mitochondrial 2-ketoacid dehydrogenases with lipoic acid, facilitating enzymatic functions involved in the tricarboxylic acid cycle. Inhibiting lipoylation, either through genetic LIPT1 knockout or a lipoylation inhibitor (CPI-613), enhanced tumor control by radiation. Mechanistically, lipoylation inhibition increased 2-hydroxyglutarate, leading to H3K9 trimethylation, disrupting TIP60 recruitment and ataxia telangiectasia mutated (ATM)-mediated DNA damage repair signaling, impairing homologous recombination repair. In summary, our findings reveal a critical role of LIPT1 in regulating DNA damage and chromosome stability and may suggest a means to enhance therapeutic outcomes with DNA-damaging agents.

MeSH terms

  • Acyltransferases / genetics
  • Acyltransferases / metabolism
  • Animals
  • Ataxia Telangiectasia Mutated Proteins / metabolism
  • CRISPR-Cas Systems
  • Carcinoma, Non-Small-Cell Lung* / genetics
  • Carcinoma, Non-Small-Cell Lung* / metabolism
  • Carcinoma, Non-Small-Cell Lung* / pathology
  • Carcinoma, Non-Small-Cell Lung* / radiotherapy
  • Cell Line, Tumor
  • DNA Damage
  • Histones / metabolism
  • Humans
  • Lipoylation* / drug effects
  • Lung Neoplasms* / genetics
  • Lung Neoplasms* / metabolism
  • Lung Neoplasms* / pathology
  • Lung Neoplasms* / radiotherapy
  • Mice
  • Recombinational DNA Repair* / drug effects
  • Recombinational DNA Repair* / radiation effects

Substances

  • Acyltransferases
  • Histones
  • Ataxia Telangiectasia Mutated Proteins