Mimicking the Nucleosomal Context in Peptide-Based Binders of a H3K36me Reader Increases Binding Affinity While Altering the Binding Mode

V Horn, SAK Jongkees, H van Ingen - Molecules, 2020 - mdpi.com
Targeting of proteins in the histone modification machinery has emerged as a promising
new direction to fight disease. The search for compounds that inhibit proteins that readout …

[PDF][PDF] The effect of the length of histone H3K4me3 on recognition by reader proteins

B Pieters, R Belle, J Mecinovic - ChemBioChem, 2013 - repository.ubn.ru.nl
Objective: Short histone 3 peptides are often used for experiments with proteins that
recognize trimethylated lysine on histone 3 (H3K4me3). In this chapter it is investigated what …

Engineered reader proteins for enhanced detection of methylated lysine on histones

KI Albanese, MW Krone, CJ Petell… - ACS chemical …, 2019 - ACS Publications
Histone post-translational modifications (PTMs) are crucial for many cellular processes
including mitosis, transcription, and DNA repair. The cellular readout of histone PTMs is …

Manipulating Cation− π Interactions of Reader Proteins in Living Cells with Genetic Code Expansion

H Zhao, L Tang, Y Fang, C Liu, W Ding… - Journal of the …, 2023 - ACS Publications
Despite tremendous success in understanding the chemical nature and the importance of
cation− π interactions in a range of biological processes, particularly in epigenetic …

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 …

Fragment Ligands of the m6A-RNA Reader YTHDF2

F Nai, R Nachawati, F Zalesak, X Wang… - ACS Medicinal …, 2022 - ACS Publications
We report 17 small-molecule ligands that compete with N6-methyladenosine (m6A) for
binding to the m6A-reader domain of YTHDF2 (YT521-B homology domain family 2). We …

[HTML][HTML] A degenerate peptide library approach to reveal sequence determinants of methyllysine-driven protein interactions

A Kupai, RM Vaughan, BM Dickson… - Frontiers in Cell and …, 2020 - frontiersin.org
Lysine methylation facilitates protein-protein interactions through the activity of methyllysine
(Kme)“reader” proteins. Functions of Kme readers have historically been studied in the …

PROBING THE DEGRADABILITY OF METHYL-LYSINE READER PROTEINS USING HETEROBIFUNCTIONAL MOLECULES

KB Guzman Rodriguez - 2021 - cdr.lib.unc.edu
Methyl-lysine reader (Kme) proteins recognize post-translational modifications, specifically
methyl marks, on histone tails and recruit other chromatin interacting proteins that participate …

Probing the Degradability of Methyl-Lysine Reader Proteins Using Heterobifunctional Molecules

KBG Rodriguez - 2021 - search.proquest.com
Methyl-lysine reader (Kme) proteins recognize post-translational modifications, specifically
methyl marks, on histone tails and recruit other chromatin interacting proteins that participate …

Improved methods for targeting epigenetic reader domains of acetylated and methylated lysine

IA Engelberg, CA Foley, LI James, SV Frye - Current opinion in chemical …, 2021 - Elsevier
Responsible for interpreting histone post-translational modifications, epigenetic reader
proteins have emerged as novel therapeutic targets for a wide range of diseases. Chemical …