Condensate-Promoting ENL Mutation Drives Tumorigenesis In Vivo Through Dynamic Regulation of Histone Modifications and Gene Expression

Y Liu, Q Li, L Song, C Gong, S Tang… - Cancer …, 2024 - aacrjournals.org
Gain-of-function mutations in the histone acetylation “reader” eleven-nineteen-leukemia
(ENL), found in acute myeloid leukemia (AML) and Wilms tumor, are known to drive …

Automated CUT&Tag profiling of chromatin heterogeneity in mixed-lineage leukemia

DH Janssens, MP Meers, SJ Wu, E Babaeva… - Nature …, 2021 - nature.com
Acute myeloid and lymphoid leukemias often harbor chromosomal translocations involving
the KMT2A gene, encoding the KMT2A lysine methyltransferase (also known as mixed …

High-resolution characterization of gene function using single-cell CRISPR tiling screen

L Yang, AKN Chan, K Miyashita, CD Delaney… - Nature …, 2021 - nature.com
Identification of novel functional domains and characterization of detailed regulatory
mechanisms in cancer-driving genes is critical for advanced cancer therapy. To date …

The role of protein acetylation in carcinogenesis and targeted drug discovery

J Yang, C Song, X Zhan - Frontiers in Endocrinology, 2022 - frontiersin.org
Protein acetylation is a reversible post-translational modification, and is involved in many
biological processes in cells, such as transcriptional regulation, DNA damage repair, and …

CDYL1-dependent decrease in lysine crotonylation at DNA double-strand break sites functionally uncouples transcriptional silencing and repair

ER Abu-Zhayia, LA Bishara, FE Machour, AS Barisaac… - Molecular Cell, 2022 - cell.com
Previously, we showed that CDYL1 is recruited to DNA double-strand breaks (DSBs) to
promote homologous recombination (HR) repair and foster transcriptional silencing …

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 …

Click chemistry and targeted degradation: a winning combination for medicinal chemists?

A Pasieka, E Diamanti, E Uliassi… - …, 2023 - Wiley Online Library
Click chemistry is universally recognized as a powerful strategy for the fast and precise
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …

Integrative chemical biology approaches to deciphering the histone code: a problem-driven journey

X Li, XD Li - Accounts of chemical research, 2021 - ACS Publications
Conspectus The hereditary blueprint of a eukaryotic cell is encoded in its genomic DNA that
is tightly compacted into chromatin together with histone proteins. The basic repeating units …

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 …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …