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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 …
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 …
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 …
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
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 …
nuclear protein with histone demethylase activity. In particular, it plays a special role in the …
Structural basis of sirtuin 6-catalyzed nucleosome deacetylation
The reversible acetylation of histone lysine residues is controlled by the action of
acetyltransferases and deacetylases (HDACs), which regulate chromatin structure and gene …
acetyltransferases and deacetylases (HDACs), which regulate chromatin structure and gene …
The chemical biology of reversible lysine post-translational modifications
Lysine (Lys) residues in proteins undergo a wide range of reversible post-translational
modifications (PTMs), which can regulate enzyme activities, chromatin structure, protein …
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 …
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 …
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 …
subunits within seven distinct multiprotein corepressor complexes and are established drug …
PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes
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 …
The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the …