Histone H3K9 Lactylation Confers Temozolomide Resistance in Glioblastoma via LUC7L2-Mediated MLH1 Intron Retention

Histone H3K9 Lactylation Confers Temozolomide Resistance in Glioblastoma via LUC7L2-Mediated MLH1 Intron Retention

2024 | Qu Yue, Zhao Wang, Yixiong Shen, Yufei Lan, Xiangyang Zhong, Xin Luo, Tao Yang, Manqing Zhang, Borning Zuo, Tianci Zeng, Jiankun Lu, Yuankai Wang, Boyang Liu, Hongbo Guo
This study investigates the role of histone H3K9 lactylation (H3K9la) in temozolomide (TMZ) resistance in glioblastoma (GBM). The authors found that H3K9la is upregulated in recurrent GBM tissues and TMZ-resistant cells, and it is primarily concentrated in histone H3K9. Multi-omics analysis, including CUT&Tag, SLAM-seq, and RNA-seq, revealed that H3K9la is enriched in the LUC7L2 promoter and activates LUC7L2 transcription, which in turn mediates intron 7 retention of MLH1, reducing MLH1 expression and inhibiting mismatch repair (MMR). This results in TMZ resistance in GBM. Notably, the anti-epileptic drug stiripentol, which can cross the blood-brain barrier and inhibit lactate dehydrogenase A/B (LDHA/B) activity, acts as a lactylation inhibitor and enhances the sensitivity of GBM cells to TMZ both in vitro and in vivo. These findings provide insights into the mechanism of lactylation in TMZ resistance and suggest a potential combined therapeutic strategy for clinical GBM treatment.This study investigates the role of histone H3K9 lactylation (H3K9la) in temozolomide (TMZ) resistance in glioblastoma (GBM). The authors found that H3K9la is upregulated in recurrent GBM tissues and TMZ-resistant cells, and it is primarily concentrated in histone H3K9. Multi-omics analysis, including CUT&Tag, SLAM-seq, and RNA-seq, revealed that H3K9la is enriched in the LUC7L2 promoter and activates LUC7L2 transcription, which in turn mediates intron 7 retention of MLH1, reducing MLH1 expression and inhibiting mismatch repair (MMR). This results in TMZ resistance in GBM. Notably, the anti-epileptic drug stiripentol, which can cross the blood-brain barrier and inhibit lactate dehydrogenase A/B (LDHA/B) activity, acts as a lactylation inhibitor and enhances the sensitivity of GBM cells to TMZ both in vitro and in vivo. These findings provide insights into the mechanism of lactylation in TMZ resistance and suggest a potential combined therapeutic strategy for clinical GBM treatment.
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[slides and audio] Histone H3K9 Lactylation Confers Temozolomide Resistance in Glioblastoma via LUC7L2%E2%80%90Mediated MLH1 Intron Retention