A systematic review of histone lysine‐specific demethylase 1 and its inhibitors

YC Zheng, J Ma, Z Wang, J Li, B Jiang… - Medicinal research …, 2015 - Wiley Online Library
Histone lysine‐specific demethylase 1 (LSD1) is the first discovered and reported histone
demethylase by Dr. Shi Yang's group in 2004. It is classified as a member of amine oxidase …

Reversible inhibitors of LSD1 as therapeutic agents in acute myeloid leukemia: clinical significance and progress to date

DP Mould, AE McGonagle, DH Wiseman… - Medicinal research …, 2015 - Wiley Online Library
In the 10 years since the discovery of lysine‐specific demethylase 1 (LSD1), this epigenetic
eraser has emerged as an important target of interest in oncology. More specifically …

Triazole–dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration

YC Zheng, YC Duan, JL Ma, RM Xu, X Zi… - Journal of medicinal …, 2013 - ACS Publications
Lysine specific demethylase 1 (LSD1), the first identified histone demethylase, plays an
important role in epigenetic regulation of gene activation and repression. The up-regulated …

Structural and functional landscape of FAD-dependent histone lysine demethylases for new drug discovery

Y Song, S Wang, B Yu - Journal of Medicinal Chemistry, 2022 - ACS Publications
Small molecules targeting the flavin adenine dinucleotide (FAD)-dependent histone lysine
demethylase LSD family have displayed therapeutic promise against various diseases. Nine …

Protein–protein interactions mediated by helical tertiary structure motifs

AM Watkins, MG Wuo, PS Arora - Journal of the American …, 2015 - ACS Publications
The modulation of protein–protein interactions (PPIs) by means of creating or stabilizing
secondary structure conformations is a rapidly growing area of research. Recent success in …

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 …

KDM1A microenvironment, its oncogenic potential, and therapeutic significance

T Ismail, HK Lee, C Kim, T Kwon, TJ Park… - Epigenetics & …, 2018 - Springer
The lysine-specific histone demethylase 1A (KDM1A) was the first demethylase to challenge
the concept of the irreversible nature of methylation marks. KDM1A, containing a flavin …

KDM1 class flavin‐dependent protein lysine demethylases

JM Burg, JE Link, BS Morgan, FJ Heller… - Peptide …, 2015 - Wiley Online Library
Flavin‐dependent, lysine‐specific protein demethylases (KDM1s) are a subfamily of amine
oxidases that catalyze the selective posttranslational oxidative demethylation of methyllysine …

Epigenetic drug discovery: a success story for cofactor interference

A Ganesan - … Transactions of the Royal Society B …, 2018 - royalsocietypublishing.org
Within the past two decades, seven epigenetic drugs have received regulatory approval and
numerous other candidates are currently in clinical trials. Among the epigenetic targets are …

CoREST complex-selective histone deacetylase inhibitors show prosynaptic effects and an improved safety profile to enable treatment of synaptopathies

NO Fuller, A Pirone, BA Lynch, MC Hewitt… - ACS Chemical …, 2018 - ACS Publications
Synaptic dysfunction is a pathological feature in many neurodegenerative disorders,
including Alzheimer's disease, and synaptic loss correlates closely with cognitive decline …