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 …

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 …

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 …

Tranylcypromine based lysine-specific demethylase 1 inhibitor: summary and perspective

XJ Dai, Y Liu, XP Xiong, LP Xue… - Journal of Medicinal …, 2020 - ACS Publications
Histone lysine-specific demethylase 1 (LSD1/KDM1A) has become an important and
promising anticancer target since it was first identified in 2004 and specially demethylates …

Therapeutic potential of targeting LSD1/KDM1A in cancers

X Zhang, X Wang, T Wu, W Yin, J Yan, Y Sun… - Pharmacological …, 2022 - Elsevier
LSD1 was the first histone demethylase identified by Professor Shi Yang and his team
members in 2004. LSD1 employs FAD as its cofactor, which catalyzes the demethylation of …

A novel LSD1 inhibitor T-3775440 disrupts GFI1B-containing complex leading to transdifferentiation and impaired growth of AML cells

Y Ishikawa, K Gamo, M Yabuki, S Takagi… - Molecular cancer …, 2017 - AACR
Dysregulation of lysine (K)-specific demethylase 1A (LSD1), also known as KDM1A, has
been implicated in the development of various cancers, including leukemia. Here, we …

Kinetics, mechanism, and inhibition of monoamine oxidase

RR Ramsay, A Albreht - Journal of Neural Transmission, 2018 - Springer
Monoamine oxidases (MAOs) catalyse the oxidation of neurotransmitter amines and a wide
variety of primary, secondary and tertiary amine xenobiotics, including therapeutic drugs …

A comprehensive comparative study on LSD1 in different cancers and tumor specific LSD1 inhibitors

J Dong, W Pervaiz, B Tayyab, D Li, L Kang… - European journal of …, 2022 - Elsevier
LSD1 was significantly over-expressed in several cancer types, and its aberrant
overexpression was revealed to play a crucial role in the initiation and progression of …

Irreversible LSD1 inhibitors: application of tranylcypromine and its derivatives in cancer treatment

Y C. Zheng, B Yu, G Z. Jiang, X J. Feng… - Current topics in …, 2016 - benthamdirect.com
Due to the increasing costs and time consuming for new drug discovery, a large number of
pharmaceutical firms have chosen to modify the existing drug molecules for repositioning …

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 …