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 …
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 …
LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials
B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …
[HTML][HTML] Histone tail conformations: a fuzzy affair with DNA
M Ghoneim, HA Fuchs, CA Musselman - Trends in biochemical sciences, 2021 - cell.com
The core histone tails are critical in chromatin structure and signaling. Studies over the past
several decades have provided a wealth of information on the histone tails and their …
several decades have provided a wealth of information on the histone tails and their …
Mechanism of crosstalk between the LSD1 demethylase and HDAC1 deacetylase in the CoREST complex
The transcriptional corepressor complex CoREST is one of seven histone deacetylase
complexes that regulate the genome through controlling chromatin acetylation. The CoREST …
complexes that regulate the genome through controlling chromatin acetylation. The CoREST …
Histone demethylases in chromatin biology and beyond
E Dimitrova, AH Turberfield, RJ Klose - EMBO reports, 2015 - embopress.org
Histone methylation plays fundamental roles in regulating chromatin‐based processes. With
the discovery of histone demethylases over a decade ago, it is now clear that histone …
the discovery of histone demethylases over a decade ago, it is now clear that histone …
Pharmacological inhibition of LSD1 for cancer treatment
GJ Yang, PM Lei, SY Wong, DL Ma, CH Leung - Molecules, 2018 - mdpi.com
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …
Crystal structure of the LSD1/CoREST histone demethylase bound to its nucleosome substrate
LSD1 (lysine specific demethylase; also known as KDM1A), the first histone demethylase
discovered, regulates cell-fate determination and is overexpressed in multiple cancers …
discovered, regulates cell-fate determination and is overexpressed in multiple cancers …
Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1
Biochemical crosstalk between two or more histone modifications is often observed in
epigenetic enzyme regulation, but its functional significance in cells has been difficult to …
epigenetic enzyme regulation, but its functional significance in cells has been difficult to …
CRISPR-suppressor scanning reveals a nonenzymatic role of LSD1 in AML
ME Vinyard, C Su, AP Siegenfeld, AL Waterbury… - Nature chemical …, 2019 - nature.com
Understanding the mechanism of small molecules is a critical challenge in chemical biology
and drug discovery. Medicinal chemistry is essential for elucidating drug mechanism …
and drug discovery. Medicinal chemistry is essential for elucidating drug mechanism …