Targeting epigenetic regulators to overcome drug resistance in cancers

N Wang, T Ma, B Yu - Signal transduction and targeted therapy, 2023 - nature.com
Drug resistance is mainly responsible for cancer recurrence and poor prognosis. Epigenetic
regulation is a heritable change in gene expressions independent of nucleotide sequence …

[HTML][HTML] Histone deacetylases (HDACs): evolution, specificity, role in transcriptional complexes, and pharmacological actionability

G Milazzo, D Mercatelli, G Di Muzio, L Triboli… - Genes, 2020 - mdpi.com
Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by
removing acetyl groups from histones and other protein regulatory factors, with functional …

Class I histone deacetylases (HDAC1–3) are histone lysine delactylases

C Moreno-Yruela, D Zhang, W Wei, M Bæk, W Liu… - Science …, 2022 - science.org
Lysine L-lactylation [K (L-la)] is a newly discovered histone mark stimulated under conditions
of high glycolysis, such as the Warburg effect. K (L-la) is associated with functions that are …

LSD1: more than demethylation of histone lysine residues

B Perillo, A Tramontano, A Pezone… - Experimental & molecular …, 2020 - nature.com
Lysine-specific histone demethylase 1 (LSD1) represents the first example of an identified
nuclear protein with histone demethylase activity. In particular, it plays a special role in the …

Structural basis of sirtuin 6-catalyzed nucleosome deacetylation

ZA Wang, JW Markert, SD Whedon… - Journal of the …, 2023 - ACS Publications
The reversible acetylation of histone lysine residues is controlled by the action of
acetyltransferases and deacetylases (HDACs), which regulate chromatin structure and gene …

The chemical biology of reversible lysine post-translational modifications

ZA Wang, PA Cole - Cell chemical biology, 2020 - cell.com
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …

[HTML][HTML] Beamline B21: high-throughput small-angle X-ray scattering at Diamond Light Source

NP Cowieson, CJC Edwards-Gayle, K Inoue… - Synchrotron …, 2020 - journals.iucr.org
B21 is a small-angle X-ray scattering (SAXS) beamline with a bending magnet source in the
3 GeV storage ring at the Diamond Light Source Ltd synchrotron in the UK. The beamline …

Histone deacetylase complexes: Structure, regulation and function

MD Asmamaw, A He, LR Zhang, HM Liu… - Biochimica et Biophysica …, 2024 - Elsevier
Histone deacetylases (HDACs) are key epigenetic regulators, and transcriptional complexes
with deacetylase function are among the epigenetic corepressor complexes in the nucleus …

Optimization of class I histone deacetylase PROTACs reveals that HDAC1/2 degradation is critical to induce apoptosis and cell arrest in cancer cells

JP Smalley, IM Baker, WA Pytel, LY Lin… - Journal of medicinal …, 2022 - ACS Publications
Class I histone deacetylase (HDAC) enzymes 1, 2, and 3 organize chromatin as the catalytic
subunits within seven distinct multiprotein corepressor complexes and are established drug …

PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes

KS James, WR John, S MichaeláCowley - Chemical …, 2020 - pubs.rsc.org
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3.
The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the …