Deubiquitylating enzymes and drug discovery: emerging opportunities

JA Harrigan, X Jacq, NM Martin… - Nature reviews Drug …, 2018 - nature.com
More than a decade after a Nobel Prize was awarded for the discovery of the ubiquitin–
proteasome system and clinical approval of proteasome and ubiquitin E3 ligase inhibitors …

Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress

ME Neganova, SG Klochkov, YR Aleksandrova… - Seminars in Cancer …, 2022 - Elsevier
Epigenetic changes associated with histone modifications play an important role in the
emergence and maintenance of the phenotype of various cancer types. In contrast to direct …

A CRISPR dropout screen identifies genetic vulnerabilities and therapeutic targets in acute myeloid leukemia

K Tzelepis, H Koike-Yusa, E De Braekeleer, Y Li… - Cell reports, 2016 - cell.com
Acute myeloid leukemia (AML) is an aggressive cancer with a poor prognosis, for which
mainstream treatments have not changed for decades. To identify additional therapeutic …

KAT2A coupled with the α-KGDH complex acts as a histone H3 succinyltransferase

Y Wang, YR Guo, K Liu, Z Yin, R Liu, Y Xia, L Tan… - Nature, 2017 - nature.com
Histone modifications, such as the frequently occurring lysine succinylation,, are central to
the regulation of chromatin-based processes. However, the mechanism and functional …

Acetylation on histone H3 lysine 9 mediates a switch from transcription initiation to elongation

LA Gates, J Shi, AD Rohira, Q Feng, B Zhu… - Journal of Biological …, 2017 - ASBMB
The transition from transcription initiation to elongation is a key regulatory step in gene
expression, which requires RNA polymerase II (pol II) to escape promoter proximal pausing …

USP44 regulates irradiation-induced DNA double-strand break repair and suppresses tumorigenesis in nasopharyngeal carcinoma

Y Chen, Y Zhao, X Yang, X Ren, S Huang… - Nature …, 2022 - nature.com
Radiotherapy is the primary treatment for patients with nasopharyngeal carcinoma (NPC),
and approximately 20% of patients experience treatment failure due to tumour …

The existence of a nonclassical TCA cycle in the nucleus that wires the metabolic-epigenetic circuitry

X Liu, W Si, L He, J Yang, Y Peng, J Ren… - Signal transduction and …, 2021 - nature.com
The scope and variety of the metabolic intermediates from the mitochondrial tricarboxylic
acid (TCA) cycle that are engaged in epigenetic regulation of the chromatin function in the …

Glutarylation of histone H4 lysine 91 regulates chromatin dynamics

X Bao, Z Liu, W Zhang, K Gladysz, YME Fung, G Tian… - Molecular cell, 2019 - cell.com
Histone posttranslational modifications (PTMs) regulate chromatin structure and dynamics
during various DNA-associated processes. Here, we report that lysine glutarylation (Kglu) …

YEATS2 links histone acetylation to tumorigenesis of non-small cell lung cancer

W Mi, H Guan, J Lyu, D Zhao, Y Xi, S Jiang… - Nature …, 2017 - nature.com
Recognition of modified histones by “reader” proteins constitutes a key mechanism
regulating diverse chromatin-associated processes important for normal and neoplastic …

Structure of the human SAGA coactivator complex

DA Herbst, MN Esbin, RK Louder… - Nature structural & …, 2021 - nature.com
The SAGA complex is a regulatory hub involved in gene regulation, chromatin modification,
DNA damage repair and signaling. While structures of yeast SAGA (ySAGA) have been …