Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

Principles of nucleosome recognition by chromatin factors and enzymes

RK McGinty, S Tan - Current Opinion in Structural Biology, 2021 - Elsevier
The recent torrent of structures of chromatin complexes determined by cryoelectron
microscopy provides an opportunity to discern general principles for how chromatin factors …

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 …

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 …

Demethylase-independent roles of LSD1 in regulating enhancers and cell fate transition

C Zeng, J Chen, EW Cooke, A Subuddhi… - Nature …, 2023 - nature.com
The major enhancer regulator lysine-specific histone demethylase 1A (LSD1) is required for
mammalian embryogenesis and is implicated in human congenital diseases and multiple …

Reversible lysine specific demethylase 1 (LSD1) inhibitors: a promising wrench to impair LSD1

XJ Dai, Y Liu, LP Xue, XP Xiong, Y Zhou… - Journal of medicinal …, 2021 - ACS Publications
As a flavin adenine dinucleotide (FAD)-dependent monoamine oxidase, lysine specific
demethylase 1 (LSD1/KDM1A) functions as a transcription coactivator or corepressor to …

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 …

The scaffolding function of LSD1 controls DNA methylation in mouse ESCs

S Malla, K Kumari, CA García-Prieto, J Caroli… - Nature …, 2024 - nature.com
Lysine-specific histone demethylase 1 (LSD1), which demethylates mono-or di-methylated
histone H3 on lysine 4 (H3K4me1/2), is essential for early embryogenesis and development …

LSD1: expanding functions in stem cells and differentiation

C Martinez-Gamero, S Malla, F Aguilo - Cells, 2021 - mdpi.com
Embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSC) provide a powerful
model system to uncover fundamental mechanisms that control cellular identity during …

Repression of LSD1 potentiates homologous recombination-proficient ovarian cancer to PARP inhibitors through down-regulation of BRCA1/2 and RAD51

L Tao, Y Zhou, X Pan, Y Luo, J Qiu, X Zhou… - Nature …, 2023 - nature.com
Poly (ADP-ribose) polymerase inhibitors (PARPi) are selectively active in ovarian cancer
(OC) with homologous recombination (HR) deficiency (HRD) caused by mutations in …