The Jumonji C (JmjC) domain containing histone lysine demethylases have a clear role both in the development and in some diseases including inflammation and cancer. The histone lysine demethylases represent an attractive target for the identification of therapeutic agents and the pyridine derivatives are a scaffolds largely investigated for the identification and development of inhibitors of enzymes of the Jumonji family. This commentary is a scientific evaluation of a patent application US20160102096A1 that describes novel pyridine derivatives in which the introduction of specific substituents is used to modulate the selectivity profile of the inhibitors.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1080/13543776.2016.1246539 | DOI Listing |
Transcriptional silencers are -regulatory elements that downregulate the expression of target genes. Although thousands of silencers have been identified experimentally, a predictive chromatin signature of silencers has not been found. H4K20me1 previously was reported to be highly enriched among human silencers, but our reanalysis of those data using an appropriate background revealed that the enrichment is only marginal.
View Article and Find Full Text PDFAnal Chem
January 2025
Shanghai Key Laboratory of Functional Materials Chemistry, School of Chemistry and Molecular Engineering, East China University of Science and Technology, Meilong Road, Shanghai 200237, P. R. China.
Protein methylation has attracted increasing attention due to its significant regulatory roles in various biological processes. However, the diversity of methylation forms, subtle differences between methylated and nonmodified sites, and their ultralow abundances pose substantial challenges for capturing and isolating methylated peptides from biological samples. Herein, we develop a chromatographic method that utilizes 4-sulfonylcalix[4]arene (SC4A) as a mobile phase additive and Click-Maltose as the stationary phase to separate methylated/nonmethylated peptides through the adsorption of the SC4A-(Me3) complex.
View Article and Find Full Text PDFCancer Lett
January 2025
Advanced Medical Research Institute, Qilu College of Medicine, Shandong University, Jinan, 250012, China. Electronic address:
Dysregulated lipid metabolism is linked to tumor progression. In this study, we identified Niemann-Pick C1-like 1 (NPC1L1) as a downstream effector of PKM2. In breast cancer cells, PKM2 knockout (KO) enhanced NPC1L1 expression while downregulating peroxisome proliferator-activated receptor α (PPARα) signaling pathway.
View Article and Find Full Text PDFMolecules
January 2025
Department of Experimental Medicine, Sapienza University of Rome, 00161 Rome, Italy.
Epigenetic abnormalities play a critical role in colon carcinogenesis, making them a promising target for therapeutic interventions. In this study, we demonstrated that curcumin reduces colon cancer cell survival and that a decrease in lysine methylation was involved in such an effect. This correlated with the downregulation of methyltransferases EZH2, MLL1, and G9a, in both wild-type p53 (wtp53) HCT116 cells and mutant p53 (mutp53) SW480 cells, as well as SET7/9 specifically in wtp53 HCT116 cells.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
School of Life Science, Northwest University, Xi'an 710069, China.
Breast cancer (BC) subtypes exhibit distinct epigenetic landscapes, with triple-negative breast cancer (TNBC) lacking effective targeted therapies. This study investigates histone biomarkers and therapeutic vulnerabilities across BC subtypes. The immunohistochemical profiling of >20 histone biomarkers, including histone modifications, modifiers, and oncohistone mutations, was conducted on a discovery cohort and a validation cohort of BC tissues, healthy controls, and cell line models.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!