Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

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 …

CETSA and thermal proteome profiling strategies for target identification and drug discovery of natural products

Y Tu, L Tan, H Tao, Y Li, H Liu - Phytomedicine, 2023 - Elsevier
Background Monitoring target engagement at various stages of drug development is
essential for natural product (NP)-based drug discovery and development. The cellular …

Small-molecule inhibition of the acyl-lysine reader ENL as a strategy against acute myeloid leukemia

Y Liu, Q Li, F Alikarami, DR Barrett, L Mahdavi, H Li… - Cancer discovery, 2022 - AACR
The chromatin reader eleven–nineteen leukemia (ENL) has been identified as a critical
dependency in acute myeloid leukemia (AML), but its therapeutic potential remains unclear …

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 …

TAZ/YAP fusion proteins: Mechanistic insights and therapeutic opportunities

K Garcia, AC Gingras, KF Harvey, MR Tanas - Trends in cancer, 2022 - cell.com
The Hippo pathway is dysregulated in many different cancers, but point mutations in the
pathway are rare. Transcriptional co-activator with PDZ-binding motif (TAZ) and Yes …

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 …

Validating small molecule chemical probes for biological discovery

V Vu, MM Szewczyk, DY Nie… - Annual review of …, 2022 - annualreviews.org
Small molecule chemical probes are valuable tools for interrogating protein biological
functions and relevance as a therapeutic target. Rigorous validation of chemical probe …

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 …

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) …