A specific assay for JmjC domain-containing lysine demethylase and its application to inhibitor screening

He, Wen; Guo, Li; Chen, Yongcan; Li, Meiting; Lv, Yafei; Li, Zhiming; Li, Yinglu; Hou, Tianyun; Wang, Hui; Liu, Chaohua; Lu, Xiaopeng; Zhu, Qian; Bao, Yantao; Liu, Ge; Li, Xiaofan; Zhu, Weiguo

doi:10.1007/s11427-019-9582-9

Cited by 1 publication

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“…The importance of histone methylation is also being demonstrated by emerging evidence that links histone methylation to disease and ageing. At present, a select group of demethylase inhibitors is being evaluated in clinical trials (Wen et al, 2019). One of the most studied inhibitors is tranylcypromine, which efficiently inhibits KDM1A by forming a covalent adduct with the FAD cofactor, and two clinical trials using tranylcypromine to cure acute myeloid leukemia and myelodysplastic syndrome are underway (Jambhekar et al, 2017).…”

Section: Perspectives and Concluding Remarksmentioning

confidence: 99%

Biological function and regulation of histone 4 lysine 20 methylation in DNA damage response

Kohi

Feng

Tian

et al. 2022

GENOME INSTAB. DIS.

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Cells are often under attack from various DNA-damaging agents. Accurate repair is required to protect cells from the genome instability induced by DNA lesions. DNA damage response (DDR) signaling involves sensitizing, transmitting, and repairing different types of damage within chromatin complexes. Chromatin is a highly ordered complex packed with repeating units of nucleosomes and linker DNA sequences. Chromatin structure, gene transcription, and various biological processes are regulated by histone post-translational modifications (PTMs), including acetylation, methylation, phosphorylation, and ubiquitylation. Of these, the involvement of lysine methylation, regulated by numerous lysine methyltransferases and demethylases, in the DDR has been extensively explored. In particular, histone 4 lysine 20 methylation is one of the most essential histone PTMs for biological processes and ensures genome integrity. In this review, we summarize the dynamics and modulations of histone lysine methylation during the DDR. We also comprehensively describe the functions, mechanisms, and regulation of H4K20 methylation and its modifying enzymes in response to DNA damage.

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Section: Perspectives and Concluding Remarksmentioning

confidence: 99%