Protein lysine crotonylation: past, present, perspective

G Jiang, C Li, M Lu, K Lu, H Li - Cell death & disease, 2021 - nature.com
Lysine crotonylation has been discovered in histone and non-histone proteins and found to
be involved in diverse diseases and biological processes, such as neuropsychiatric disease …

YEATS domains as novel epigenetic readers: structures, functions, and inhibitor development

X Li, S Liu, X Li, XD Li - ACS chemical biology, 2022 - ACS Publications
Interpretation of the histone posttranslational modifications (PTMs) by effector proteins, or
readers, is an important epigenetic mechanism to regulate gene function. YEATS domains …

A chemical toolbox for the study of bromodomains and epigenetic signaling

Q Wu, D Heidenreich, S Zhou, S Ackloo… - Nature …, 2019 - nature.com
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …

Fragment-to-lead medicinal chemistry publications in 2019

W Jahnke, DA Erlanson, IJP De Esch… - Journal of medicinal …, 2020 - ACS Publications
Fragment-based drug discovery (FBDD) has grown and matured to a point where it is
valuable to keep track of its extent and details of application. This Perspective summarizes …

Chemical inhibition of ENL/AF9 YEATS domains in acute leukemia

L Garnar-Wortzel, TR Bishop, S Kitamura… - ACS central …, 2021 - ACS Publications
Transcriptional coregulators, which mediate chromatin-dependent transcriptional signaling,
represent tractable targets to modulate tumorigenic gene expression programs with small …

Fragment-to-lead medicinal chemistry publications in 2018

DA Erlanson, IJP de Esch, W Jahnke… - Journal of medicinal …, 2020 - ACS Publications
This Perspective, the fourth in an annual series, summarizes fragment-to-lead (F2L) success
stories published during 2018. Topics such as target class, screening methods …

Discovery of high-affinity small-molecule binders of the epigenetic reader YEATS4

AT Londregan, K Aitmakhanova, J Bennett… - Journal of medicinal …, 2022 - ACS Publications
A series of small-molecule YEATS4 binders have been discovered as part of an ongoing
research effort to generate high-quality probe molecules for emerging and/or challenging …

Leveraging a Phage-Encoded Noncanonical Amino Acid: A Novel Pathway to Potent and Selective Epigenetic Reader Protein Inhibitors

PHC Chen, XS Guo, HE Zhang, GK Dubey… - ACS Central …, 2024 - ACS Publications
Epigenetic reader proteins interpret histone epigenetic marks to regulate gene expression.
Given their vital roles and the link between their dysfunction and various diseases, these …

Discovery of selective small-molecule inhibitors for the ENL YEATS domain

XR Ma, L Xu, S Xu, BJ Klein, H Wang… - Journal of medicinal …, 2021 - ACS Publications
Eleven-nineteen leukemia (ENL) protein is a histone acetylation reader essential for disease
maintenance in acute leukemias, in particular, the mixed-lineage leukemia (MLL) …

More Than π–π–π Stacking: Contribution of Amide− π and CH− π Interactions to Crotonyllysine Binding by the AF9 YEATS Domain

MW Krone, CR Travis, GY Lee, HJ Eckvahl… - Journal of the …, 2020 - ACS Publications
Lysine crotonylation (Kcr) is a histone post-translational modification that is implicated in
numerous epigenetic pathways and diseases. Recognition of Kcr by YEATS domains has …