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 …

Epigenetic polypharmacology: A new frontier for epi‐drug discovery

D Tomaselli, A Lucidi, D Rotili… - Medicinal research …, 2020 - Wiley Online Library
Recently, despite the great success achieved by the so‐called “magic bullets” in the
treatment of different diseases through a marked and specific interaction with the target of …

Epi-drugs and Epi-miRs: moving beyond current cancer therapies

R Salarinia, A Sahebkar, M Peyvandi… - Current cancer drug …, 2016 - ingentaconnect.com
Epigenetic modifications determine phenotypic characteristics in a reversible, stable and
genotype-independent manner. Epigenetic modifications mainly encompass CpG island …

Targeting the scaffolding role of LSD1 (KDM1A) poises acute myeloid leukemia cells for retinoic acid–induced differentiation

R Ravasio, E Ceccacci, L Nicosia, A Hosseini… - Science …, 2020 - science.org
The histone demethylase LSD1 is deregulated in several tumors, including leukemias,
providing the rationale for the clinical use of LSD1 inhibitors. In acute promyelocytic …

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 …

TCPs: privileged scaffolds for identifying potent LSD1 inhibitors for cancer therapy

YC Zheng, B Yu, ZS Chen, Y Liu, HM Liu - Epigenomics, 2016 - Taylor & Francis
Since the first lysine-specific demethylase (KDM), lysine-specific demethylase 1 (LSD1), was
characterized in 2004, several families of KDMs have been identified. LSD1 can specifically …

Histone lysine demethylase inhibitors

A Jambhekar, JN Anastas, Y Shi - Cold Spring …, 2017 - perspectivesinmedicine.cshlp.org
The dynamic regulation of covalent modifications to histones is essential for maintaining
genomic integrity and cell identity and is often compromised in cancer. Aberrant expression …

Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases

H Niwa, T Umehara - Epigenetics, 2017 - Taylor & Francis
Until 2004, many researchers believed that protein methylation in eukaryotic cells was an
irreversible reaction. However, the discovery of lysine-specific demethylase 1 in 2004 …

Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models

M Menna, F Fiorentino, B Marrocco, A Lucidi… - European Journal of …, 2022 - Elsevier
LSD1 is a histone lysine demethylase proposed as therapeutic target in cancer. Chemical
modifications applied at C2, C4 and/or C7 positions of the quinazoline core of the previously …