PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

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 …

Epigenetics-targeted drugs: Current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

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 …

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 …

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 …

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 …

Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins

X Li, Y Song - Journal of hematology & oncology, 2021 - Springer
Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …

[HTML][HTML] Mixed matrix membrane formation with porous metal–organic nanomaterials for CO2 capture and separation: A critical review

C Welton, F Chen, HC Zhou, S Yi - Carbon Capture Science & Technology, 2024 - Elsevier
Due to the increasingly severe global warming trend, the reduction of CO 2 emission and
carbon capture have attracted growing interest. The separation of CO 2 from gas mixtures …

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 …