The promise for histone methyltransferase inhibitors for epigenetic therapy in clinical oncology: a narrative review

HS Rugo, I Jacobs, S Sharma, F Scappaticci… - Advances in …, 2020 - Springer
Epigenetic processes are essential for normal development and the maintenance of tissue-
specific gene expression in mammals. Changes in gene expression and malignant cellular …

The role of NSD1, NSD2, and NSD3 histone methyltransferases in solid tumors

I Topchu, RP Pangeni, I Bychkov, SA Miller… - Cellular and Molecular …, 2022 - Springer
Abstract NSD1, NSD2, and NSD3 constitute the nuclear receptor-binding SET Domain
(NSD) family of histone 3 lysine 36 (H3K36) methyltransferases. These structurally similar …

Therapeutic strategies of dual-target small molecules to overcome drug resistance in cancer therapy

J Ye, J Wu, B Liu - Biochimica et Biophysica Acta (BBA)-Reviews on …, 2023 - Elsevier
Despite some advances in targeted therapeutics of human cancers, curative cancer
treatment still remains a tremendous challenge due to the occurrence of drug resistance. A …

New advances in canonical Wnt/β-catenin signaling in cancer

X Wen, Y Wu, A Awadasseid, Y Tanaka… - Cancer Management …, 2020 - Taylor & Francis
Wnt/β-catenin-mediated signaling is a key pathway regulating tissue growth and
development, and tumorigenesis, and has received increasing attention in recent years. In …

Dual EZH2 and G9a inhibition suppresses multiple myeloma cell proliferation by regulating the interferon signal and IRF4-MYC axis

K Ishiguro, H Kitajima, T Niinuma, R Maruyama… - Cell death …, 2021 - nature.com
Epigenetic mechanisms such as histone modification play key roles in the pathogenesis of
multiple myeloma (MM). We previously showed that EZH2, a histone H3 lysine 27 (H3K27) …

Emerging role of G9a in cancer stemness and promises as a therapeutic target

JR Haebe, CJ Bergin, T Sandouka, YD Benoit - Oncogenesis, 2021 - nature.com
The histone methyltransferase G9a is well-documented for its implication in neoplastic
growth. However, recent investigations have demonstrated a key involvement of this …

[HTML][HTML] G9a plays distinct roles in maintaining DNA methylation, retrotransposon silencing, and chromatin looping

Q Jiang, JYJ Ang, AY Lee, Q Cao, KY Li, KY Yip… - Cell reports, 2020 - cell.com
G9a is a lysine methyltransferase that regulates epigenetic modifications, transcription, and
genome organization. However, whether these properties are dependent on one another or …

[HTML][HTML] The roles of histone modifications in tumorigenesis and associated inhibitors in cancer therapy

Y Yang, M Zhang, Y Wang - Journal of the National Cancer Center, 2022 - Elsevier
Histone modifications are key factors in chromatin packaging, and are responsible for gene
regulation during cell fate determination and development. Abnormal alterations in histone …

Structure, activity, and function of the protein lysine methyltransferase G9a

C Poulard, LM Noureddine, L Pruvost, M Le Romancer - Life, 2021 - mdpi.com
G9a is a lysine methyltransferase catalyzing the majority of histone H3 mono-and
dimethylation at Lys-9 (H3K9), responsible for transcriptional repression events in …

Depletion of G9A attenuates imiquimod-induced psoriatic dermatitis via targeting EDAR-NF-κB signaling in keratinocyte

Z Fang, Y Wang, B Huang, X Chen, R Jiang… - Cell Death & …, 2023 - nature.com
Psoriasis is a common and recurrent inflammatory skin disease characterized by
inflammatory cells infiltration of the dermis and excessive proliferation, reduced apoptosis …