Development of a kind of RG108-Fluorescein conjugates for detection of DNA methyltransferase 1 (DNMT1) in living cells

Ruan, Minli; Cheng, Qunxian; Gong, Chaochao; Cao, Ziping; Xu, Ling; Zhang, Qian

doi:10.1016/j.ab.2020.113823

Cited by 4 publications

(2 citation statements)

References 26 publications

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“…Another bioimaging probe for intracellular DNMT1 was synthesized based on the inhibitor RG108. 127,128 Fluorescein isothiocyanate (FITC) is a versatile agent used for cell imaging by confocal microscopy and widely used in labeling different biomolecules since the isothiocyanate group can couple with amino groups in protein and peptide chains. 129 As shown in path II in Fig.…”

Section: Antibody-free or Endonuclease-free Methods For Dnmt1 Detectionmentioning

confidence: 99%

A review on recent advances in assays for DNMT1: a promising diagnostic biomarker for multiple human cancers

Yu,

Fu,

Xie

et al. 2024

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Section: Antibody-free or Endonuclease-free Methods For Dnmt1 Detectionmentioning

confidence: 99%

A review on recent advances in assays for DNMT1: a promising diagnostic biomarker for multiple human cancers

Yu,

Fu,

Xie

et al. 2024

Analyst

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“…We hope that these mechanisms of action will be helpful for the diagnosis and treatment of deafness. RG108 as DNMT1 plays a vital character in many biological behaviour [ 15 ]. Previous researches have shown that RG108 reduces oxidative DNA damage and apoptosis of auditory cells after noise exposure, and RG108 has a rescue effect on noise-induced hearing loss [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Deciphering the potential ability of RG108 in cisplatin-induced HEI-OC1 ototoxicity: a research based on RNA-seq and molecular biology experiment

et al. 2023

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Background Drug-induced hearing loss (DIHL) is very common, and seriously affects people's happiness in life. RG108 is a small molecule inhibitor. RG108 is protective against DIHL. Our purpose is to probe the incidence of RG108 on cisplatin-induced ototoxicity. Materials and methods In our research, the ototoxicity of RG108 was investigated in HEI-OC1. We observed under the microscope whether RG108 had an effect on cisplatin-induced cochlear hair cells. RNA-seq experiments were further performed to explore possible gene ontology (GO) and pathways. ROS assay was applied to supervisory the effect of RG108 on oxidative harm of auditory cells. In auditory cells, RG108 was tested for its effects on apoptosis-related proteins by Western blotting (WB). Results GO analysis showed that RG108 associated with apoptosis. KEGG analysis shows RG108 may act on PI3K-AKT signaling pathway (PASP) in hearing loss. BIOCARTA analysis showed that RG108 may affect oxidative stress by activating NRF2 pathway. ROS ascerted that RG108 could rescue oxidative harm in HEI-OC1. RG108 rescued cisplatin-induced significant increase in Bax and significant decrease in BCL2. RG108 attenuates cisplatin-induced cochlear apoptosis through upregulated phosphorylated PI3K and phosphorylated AKT and down-regulated caspase3. MTT experiments showed that both PI3K and AKT inhibitors could significantly rescue the damage caused by cisplatin to HEI-OC1. RG108 significantly increases the level of NRF2/HO-1/NQO1 in cisplatin-induced cells. Conclusion Overall, these results provide evidence that NRF2/PI3K-AKT axis may mediate RG108 in the treatment of DIHL, which provide a broader outlook on drug-induced deafness treatment.

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Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors

Liu,

Ruan,

Liu

et al. 2024

European Journal of Medicinal Chemistry

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Development of a kind of RG108-Fluorescein conjugates for detection of DNA methyltransferase 1 (DNMT1) in living cells

Cited by 4 publications

References 26 publications

A review on recent advances in assays for DNMT1: a promising diagnostic biomarker for multiple human cancers

A review on recent advances in assays for DNMT1: a promising diagnostic biomarker for multiple human cancers

Deciphering the potential ability of RG108 in cisplatin-induced HEI-OC1 ototoxicity: a research based on RNA-seq and molecular biology experiment

Identification of 3-(9H-carbazol-9-yl)-2-(1,3-dioxoisoindolin-2-yl)propanoic acids as promising DNMT1 inhibitors

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