Clinical advances in targeting epigenetics for cancer therapy

S Feng, DD De Carvalho - The FEBS journal, 2022 - Wiley Online Library
The appropriate coordination between epigenetic regulators is essential for spatial and
temporal regulation of gene expression and maintenance of cell identity. Cancer is a …

Histone methyltransferase DOT1L as a promising epigenetic target for treatment of solid tumors

E Alexandrova, A Salvati, G Pecoraro, J Lamberti… - Frontiers in …, 2022 - frontiersin.org
The histone lysine methyltransferase DOT1L (DOT1-like histone lysine methyltransferase) is
responsible for the epigenetic regulation of gene expression through specific methylation of …

Proteomic characterization of post-translational modifications in drug discovery

L Zhai, K Chen, B Hao, M Tan - Acta Pharmacologica Sinica, 2022 - nature.com
Protein post-translational modifications (PTMs), which are usually enzymatically catalyzed,
are major regulators of protein activity and involved in almost all celluar processes …

DOT1L activity affects neural stem cell division mode and reduces differentiation and ASNS expression

B Appiah, CL Fullio, C Ossola, I Bertani, E Restelli… - EMBO …, 2023 - embopress.org
Cortical neurogenesis depends on the balance between self‐renewal and differentiation of
apical progenitors (APs). Here, we study the epigenetic control of AP's division mode by …

The WDR11 complex is a receptor for acidic-cluster-containing cargo proteins

H Deng, G Jia, P Li, Y Tang, L Zhao, Q Yang, J Zhao… - Cell, 2024 - cell.com
Vesicle trafficking is a fundamental process that allows for the sorting and transport of
specific proteins (ie," cargoes") to different compartments of eukaryotic cells. Cargo …

[HTML][HTML] Novel insights into histone lysine methyltransferases in cancer therapy: From epigenetic regulation to selective drugs

Q Liao, J Yang, S Ge, P Chai, J Fan, R Jia - Journal of Pharmaceutical …, 2023 - Elsevier
The reversible and precise temporal and spatial regulation of histone lysine
methyltransferases (KMTs) is essential for epigenome homeostasis. The dysregulation of …

[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 …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …

Post-translational modifications that drive prostate cancer progression

I Samaržija - Biomolecules, 2021 - mdpi.com
While a protein primary structure is determined by genetic code, its specific functional form is
mostly achieved in a dynamic interplay that includes actions of many enzymes involved in …

The role of histone modification in DNA replication-coupled Nucleosome Assembly and Cancer

Y Zhang, Q Zhang, Y Zhang, J Han - International Journal of Molecular …, 2023 - mdpi.com
Histone modification regulates replication-coupled nucleosome assembly, DNA damage
repair, and gene transcription. Changes or mutations in factors involved in nucleosome …