Pharmacological inhibition of LSD1 for cancer treatment

GJ Yang, PM Lei, SY Wong, DL Ma, CH Leung - Molecules, 2018 - mdpi.com
Lysine-specific demethylase 1A (LSD1, also named KDM1A) is a demethylase that can
remove methyl groups from histones H3K4me1/2 and H3K9me1/2. It is aberrantly expressed …

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 …

Enhancer activation by pharmacologic displacement of LSD1 from GFI1 induces differentiation in acute myeloid leukemia

A Maiques-Diaz, GJ Spencer, JT Lynch, F Ciceri… - Cell reports, 2018 - cell.com
Pharmacologic inhibition of LSD1 promotes blast cell differentiation in acute myeloid
leukemia (AML) with MLL translocations. The assumption has been that differentiation is …

Targeting LSD1 for acute myeloid leukemia (AML) treatment

S Zhang, M Liu, Y Yao, B Yu, H Liu - Pharmacological research, 2021 - Elsevier
Targeted therapy for acute myeloid leukemia (AML) is an effective strategy, but currently
there are very limited therapeutic targets for AML treatment. Histone lysine specific …

Pharmacological inhibition of KDM5A for cancer treatment

GJ Yang, J Wu, L Miao, MH Zhu, QJ Zhou, XJ Lu… - European Journal of …, 2021 - Elsevier
Lysine-specific demethylase 5A (KDM5A, also named RBP2 or JARID1A) is a demethylase
that can remove methyl groups from histones H3K4me1/2/3. It is aberrantly expressed in …

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 …

Lysine-Specific Demethylase 1 Inhibitors: A Comprehensive Review Utilizing Computer-Aided Drug Design Technologies

D Han, J Lu, B Fan, W Lu, Y Xue, M Wang, T Liu, S Cui… - Molecules, 2024 - mdpi.com
Lysine-specific demethylase 1 (LSD1/KDM1A) has emerged as a promising therapeutic
target for treating various cancers (such as breast cancer, liver cancer, etc.) and other …

Discovery of new potent lysine specific histone demythelase-1 inhibitors (LSD-1) using structure based and ligand based molecular modelling and machine learning

SJ Alabed, M Zihlif, M Taha - RSC advances, 2022 - pubs.rsc.org
Lysine-specific histone demethylase 1 (LSD-1) is an epigenetic enzyme that oxidatively
cleaves methyl groups from monomethyl and dimethyl Lys4 of histone H3 and is highly …

LSD1-Based Reversible Inhibitors Virtual Screening and Binding Mechanism Computational Study

Z Yin, S Liu, X Yang, M Chen, J Du, H Liu, L Yang - Molecules, 2023 - mdpi.com
As one of the crucial targets of epigenetics, histone lysine-specific demethylase 1 (LSD1) is
significant in the occurrence and development of various tumors. Although several …

Pharmacoepigenetic processors: epigenetic drugs, drug resistance, toxicoepigenetics, and nutriepigenetics

R Cacabelos, JC Carril, A Sanmartín, P Cacabelos - Pharmacoepigenetics, 2019 - Elsevier
The pharmacoepigenetic apparatus is integrated by gene clusters of different categories,
including (i) pathogenic genes involved in disease pathogenesis,(ii) mechanistic genes …