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 …
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 …
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 …
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 …
(SPIN1) involving the process of spindle organization and chromosomal stability serves as …
Systematic profiling of histone readers in Arabidopsis thaliana
Histone post-translational modifications (PTMs) and their recognition by histone readers
exert crucial functions in eukaryotes. Despite extensive studies, conservation and diversity of …
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 …
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
Chemical modifications on histones and DNA/RNA constitute a fundamental mechanism for
epigenetic regulation. These modifications often function as docking marks to recruit or …
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
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 …
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
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 …
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 …
promotes the silencing of some tumour suppressor genes and is overexpressed in many …