Synthesis and reactivity of propargylamines in organic chemistry

K Lauder, A Toscani, N Scalacci… - Chemical reviews, 2017 - ACS Publications
Propargylamines are a versatile class of compounds which find broad application in many
fields of chemistry. This review aims to describe the different strategies developed so far for …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

LSD1: biologic roles and therapeutic targeting

A Maiques-Diaz, TCP Somervaille - Epigenomics, 2016 - Taylor & Francis
LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase
activity and has since been shown to have multiple essential roles in mammalian biology …

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 …

Acetylene group, friend or foe in medicinal chemistry

TT Talele - Journal of Medicinal Chemistry, 2020 - ACS Publications
The use of an acetylene (ethynyl) group in medicinal chemistry coincides with the launch of
the Journal of Medicinal Chemistry in 1959. Since then, the acetylene group has been …

Recent progress in histone demethylase inhibitors

TE McAllister, KS England, RJ Hopkinson… - Journal of medicinal …, 2016 - ACS Publications
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with
small molecules both for the generation of probes for target exploration and for therapeutic …

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 …

A state-of-the-art review on LSD1 and its inhibitors in breast cancer: Molecular mechanisms and therapeutic significance

GJ Yang, YJ Liu, LJ Ding, F Tao, MH Zhu… - Frontiers in …, 2022 - frontiersin.org
Breast cancer (BC) is a kind of malignant cancer in women, and it has become the most
diagnosed cancer worldwide since 2020. Histone methylation is a common biological …

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 …

Computer-aided drug design in epigenetics

W Lu, R Zhang, H Jiang, H Zhang, C Luo - Frontiers in chemistry, 2018 - frontiersin.org
Epigenetic dysfunction has been widely implicated in several diseases especially cancers
thus highlights the therapeutic potential for chemical interventions in this field. With rapid …