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 …

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 …

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 …

[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 …

Mechanism of crosstalk between the LSD1 demethylase and HDAC1 deacetylase in the CoREST complex

Y Song, L Dagil, L Fairall, N Robertson, M Wu… - Cell Reports, 2020 - cell.com
The transcriptional corepressor complex CoREST is one of seven histone deacetylase
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 …

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 …

Crystal structure of the LSD1/CoREST histone demethylase bound to its nucleosome substrate

SA Kim, J Zhu, N Yennawar, P Eek, S Tan - Molecular cell, 2020 - cell.com
LSD1 (lysine specific demethylase; also known as KDM1A), the first histone demethylase
discovered, regulates cell-fate determination and is overexpressed in multiple cancers …

Uncoupling histone modification crosstalk by engineering lysine demethylase LSD1

K Lee, M Barone, AL Waterbury, H Jiang… - Nature Chemical …, 2024 - nature.com
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 …

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 …