Histone methylation related therapeutic challenge in cardiovascular diseases

Y Yang, Y Luan, RX Yuan, Y Luan - Frontiers in Cardiovascular …, 2021 - frontiersin.org
The epidemic of cardiovascular diseases (CVDs) is predicted to spread rapidly in advanced
countries accompanied by the high prevalence of risk factors. In terms of pathogenesis, the …

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 …

Uncovering New Conformational States of the Substrate Binding Pocket of LSD1 Potential for Inhibitor Design via Funnel Metadynamics

K Yang, H Liu - The Journal of Physical Chemistry B, 2023 - ACS Publications
Lysine-specific demethylase 1 (LSD1) is a promising therapeutic target for cancer therapy.
So far, over 80 crystal structures of LSD1 in different complex states have been deposited in …

Structures of chromatin modulators in complex with nucleosome

J Min, K Liu - Current Opinion in Chemical Biology, 2021 - Elsevier
The chromatin structure is dynamically regulated by many different modulators that post-
translationally modify histones, replace canonical histones with histone variants, and unwind …

Histone lysine-specific demethylase 1 regulates the proliferation of hemocytes in the oyster Crassostrea gigas

X Gu, X Qiao, S Yu, X Song, L Wang… - Frontiers in …, 2022 - frontiersin.org
Background Lysine-specific demethylase 1 (LSD1) is an essential epigenetic regulator of
hematopoietic differentiation, which can specifically mono-methylate H3K4 (H3K4me1) and …

An autoinhibitory switch of the LSD1 disordered region controls enhancer silencing

AL Waterbury, HS Kwok, C Lee, DN Narducci… - Molecular Cell, 2024 - cell.com
Transcriptional coregulators and transcription factors (TFs) contain intrinsically disordered
regions (IDRs) that are critical for their association and function in gene regulation. More …

The kinase NEK6 positively regulates LSD1 activity and accumulation in local chromatin sub-compartments

F Knodel, J Eirich, S Pinter, SA Eisler… - Communications …, 2024 - nature.com
LSD1 plays a crucial role in mammalian biology, regulated through interactions with
coregulators and post-translational modifications. Here we show that the kinase NEK6 …

Anticancer Drugs of Lysine Specific Histone Demethylase-1 (LSD1) Display Variable Inhibition on Nucleosome Substrates

D Senanayaka, D Zeng, E Deniz, IK Priyankara… - Biochemistry, 2024 - ACS Publications
Lysine specific demethylase-1 (LSD1) serves as a regulator of transcription and represents
a promising epigenetic target for anticancer treatment. LSD1 inhibitors are in clinical trials for …

Autoregulatory mechanism of enzyme activity by the nuclear localization signal of lysine-specific demethylase 1

D Senanayaka, D Zeng, S Alishiri, WJ Martin… - Journal of Biological …, 2024 - jbc.org
The N-terminal region of the human lysine-specific demethylase 1 (LSD1) has no predicted
structural elements, contains a nuclear localization signal (NLS), undergoes multiple …

Protein methylation characterization using NMR without isotopic labeling

Z Fang, T Huang, X Chai, J Zhan, Q Zhu, P Sun… - Talanta, 2024 - Elsevier
Protein methylation is crucial in epigenetics, and targeting the involved methyltransferases
shows great potential for therapeutic intervention with several inhibitors in clinical trials for …