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 …
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 …
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 …
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 …
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 …
Chemical tools targeting readers of lysine methylation
G Ortiz, TG Kutateladze, DG Fujimori - Current opinion in chemical biology, 2023 - Elsevier
Reader domains that recognize methylated lysine and arginine residues on histones play a
role in the recruitment, stabilization, and regulation of chromatin regulatory proteins …
role in the recruitment, stabilization, and regulation of chromatin regulatory proteins …
Targeting epigenetic reader domains by chemical biology
A Cipriano, G Sbardella, A Ciulli - Current Opinion in Chemical Biology, 2020 - Elsevier
Over the past years, growing interest toward post-translational modifications (PTMs) of
histones and nonhistone proteins has prompted academia and industrial research groups to …
histones and nonhistone proteins has prompted academia and industrial research groups to …
Systematic variation of both the aromatic cage and dialkyllysine via GCE-SAR reveal mechanistic insights in CBX5 reader protein binding
KM Kean, SA Baril, KN Lamb… - Journal of medicinal …, 2022 - ACS Publications
Development of inhibitors for histone methyllysine reader proteins is an active area of
research due to the importance of reader protein–methyllysine interactions in transcriptional …
research due to the importance of reader protein–methyllysine interactions in transcriptional …
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor
Y Xiong, H Greschik, C Johansson… - Journal of medicinal …, 2024 - ACS Publications
The methyl-lysine reader protein SPIN1 plays important roles in various human diseases.
However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly …
However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly …
Histone code reader SPIN1 is a promising target of cancer therapy
D Li, J Guo, R Jia - Biochimie, 2021 - Elsevier
SPIN1 is a histone methylation reader, which can epigenetically control multiple
tumorigenesis-associated signaling pathways, including the Wnt, PI3K/AKT, and RET …
tumorigenesis-associated signaling pathways, including the Wnt, PI3K/AKT, and RET …