The interplay between DNA and histone methylation: molecular mechanisms and disease implications

Y Li, X Chen, C Lu - EMBO reports, 2021 - embopress.org
Methylation of cytosine in CpG dinucleotides and histone lysine and arginine residues is a
chromatin modification that critically contributes to the regulation of genome integrity …

Epigenetics-targeted drugs: current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

Pharmacological perturbation of the phase-separating protein SMNDC1

L Enders, M Siklos, J Borggräfe, S Gaussmann… - Nature …, 2023 - nature.com
SMNDC1 is a Tudor domain protein that recognizes di-methylated arginines and controls
gene expression as an essential splicing factor. Here, we study the specific contributions of …

Defining UHRF1 domains that support maintenance of human colon cancer DNA methylation and oncogenic properties

X Kong, J Chen, W Xie, SM Brown, Y Cai, K Wu, D Fan… - Cancer Cell, 2019 - cell.com
UHRF1 facilitates the establishment and maintenance of DNA methylation patterns in
mammalian cells. The establishment domains are defined, including E3 ligase function, but …

A small molecule antagonist of SMN disrupts the interaction between SMN and RNAP II

Y Liu, A Iqbal, W Li, Z Ni, Y Wang, J Ramprasad… - Nature …, 2022 - nature.com
Survival of motor neuron (SMN) functions in diverse biological pathways via recognition of
symmetric dimethylarginine (Rme2s) on proteins by its Tudor domain, and deficiency of …

Discovery of triazinone derivatives as novel, specific, and direct NLRP3 inflammasome inhibitors for the treatment of DSS-induced ulcerative colitis

N Li, X Jiang, R Zhang, N Ye, M Tang… - Journal of Medicinal …, 2023 - ACS Publications
NLRP3 is an intracellular sensor protein that causes inflammasome formation and
pyroptosis in response to a wide range of stimuli. Aberrant activation of NLRP3 …

Targeting non-bromodomain chromatin readers

CH Arrowsmith, M Schapira - Nature structural & molecular biology, 2019 - nature.com
Chromatin regulatory proteins are increasingly recognized as potential new drug targets.
Many of these proteins harbor one or more so called 'reader domains' that recognize …

Chemical inhibitors targeting histone methylation readers

X Huang, Y Chen, Q Xiao, X Shang, Y Liu - Pharmacology & Therapeutics, 2024 - Elsevier
Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …

Targeting Alpha‐Ketoglutarate Disruption Overcomes Immunoevasion and Improves PD‐1 Blockade Immunotherapy in Renal Cell Carcinoma

L Li, X Zeng, Z Chao, J Luo, W Guan… - Advanced …, 2023 - Wiley Online Library
The Warburg effect‐related metabolic dysfunction of the tricarboxylic acid (TCA) cycle has
emerged as a hallmark of various solid tumors, particularly renal cell carcinoma (RCC). RCC …

Trimethyllysine reader proteins exhibit widespread charge-agnostic binding via different mechanisms to cationic and neutral ligands

CR Travis, KM Kean, KI Albanese… - Journal of the …, 2024 - ACS Publications
In the last 40 years, cation− π interactions have become part of the lexicon of noncovalent
forces that drive protein binding. Indeed, tetraalkylammoniums are universally bound by …