LSD1/KDM1A inhibitors in clinical trials: advances and prospects

Y Fang, G Liao, B Yu - Journal of hematology & oncology, 2019 - Springer
Histone demethylase LSD1 plays key roles during carcinogenesis, targeting LSD1 is
becoming an emerging option for the treatment of cancers. Numerous LSD1 inhibitors have …

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

XJ Dai, Y Liu, XP **ong, 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 …

Targeting epigenetic regulators with covalent small-molecule inhibitors

Y Zhang, D Rong, B Li, Y Wang - Journal of Medicinal Chemistry, 2021 - ACS Publications
Epigenetic regulation of gene expression plays a critical role in various physiological
processes, and epigenetic dysregulation is implicated in a number of diseases, prominently …

Development of (4-cyanophenyl) glycine derivatives as reversible inhibitors of lysine specific demethylase 1

DP Mould, C Alli, U Bremberg, S Cartic… - Journal of Medicinal …, 2017 - ACS Publications
Inhibition of lysine specific demethylase 1 (LSD1) has been shown to induce the
differentiation of leukemia stem cells in acute myeloid leukemia (AML). Irreversible inhibitors …

Structure-activity studies on N-substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of …

J Schulz-Fincke, M Hau, J Barth, D Robaa… - European Journal of …, 2018 - Elsevier
FAD-dependent lysine-specific demethylase 1 (LSD1) is overexpressed or deregulated in
many cancers such as AML and prostate cancer and hence is a promising anticancer target …

Epigenetic processes in Alzheimer's disease

I Castanho, K Lunnon - Chromatin signaling and neurological disorders, 2019 - Elsevier
Alzheimer's disease (AD) is the most common cause of dementia and is characterized by
memory loss and cognitive decline, which are consequences of chronic progressive …

Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors

MJ Huang, JW Guo, YD Fu, YZ You, WY Xu… - Bioorganic & Medicinal …, 2021 - Elsevier
Tranylcypromine (TCP)-based structural modifications lead to the discovery of new LSD1
inhibitors, of which compounds 26b and 29b effectively inhibit LSD1 with the IC 50 values of …

Lysine-specific histone demethylases 1/2 (LSD1/2) and their inhibitors

T Suzuki - Chemical Epigenetics, 2020 - Springer
Histone lysine methylation, one of the epigenetic mechanisms, plays a pivotal role in various
biological events, including cell cycle progression, immune response, and signal …

Method of treating multiple sclerosis employing a LSD1-inhibitor

T Maes, CM CRUSAT, DR POZO - US Patent 10,780,081, 2020 - Google Patents
US10780081B2 - Method of treating multiple sclerosis employing a LSD1-inhibitor - Google
Patents US10780081B2 - Method of treating multiple sclerosis employing a LSD1-inhibitor …