Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

HP Mohammad, O Barbash, CL Creasy - Nature medicine, 2019 - nature.com
Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

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 …

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 …

SPIN1 triggers abnormal lipid metabolism and enhances tumor growth in liver cancer

M Zhao, Y Bu, J Feng, H Zhang, Y Chen, G Yang, Z Liu… - Cancer Letters, 2020 - Elsevier
Abnormal lipid metabolism plays crucial roles in the development of cancer. Spindlin 1
(SPIN1) involving the process of spindle organization and chromosomal stability serves as …

Systematic profiling of histone readers in Arabidopsis thaliana

S Zhao, B Zhang, M Yang, J Zhu, H Li - Cell reports, 2018 - cell.com
Histone post-translational modifications (PTMs) and their recognition by histone readers
exert crucial functions in eukaryotes. Despite extensive studies, conservation and diversity of …

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 …

Kinetic and high-throughput profiling of epigenetic interactions by 3D-carbene chip-based surface plasmon resonance imaging technology

S Zhao, M Yang, W Zhou, B Zhang… - Proceedings of the …, 2017 - National Acad Sciences
Chemical modifications on histones and DNA/RNA constitute a fundamental mechanism for
epigenetic regulation. These modifications often function as docking marks to recruit or …

Contribution of Electrostatic CH3–π Interactions to Recognition of Histone Asymmetric Dimethylarginine by the SPIN1 Triple Tudor Domain

CR Travis, RG Dumais, JW Treacy… - Journal of the …, 2024 - ACS Publications
Methylation of arginine (Arg) residues on histones creates a new binding epitope, enabling
recognition by aromatic cage binding pockets in Tudor domains; these protein–protein …

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 …

Structure‐guided discovery of a potent and selective cell‐active inhibitor of SETDB1 tudor domain

Y Guo, X Mao, L Xiong, A Xia, J You… - Angewandte Chemie …, 2021 - Wiley Online Library
SET domain bifurcated protein 1 (SETDB1) is a histone lysine methyltransferase that
promotes the silencing of some tumour suppressor genes and is overexpressed in many …