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 …

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …

[HTML][HTML] Natural products as LSD1 inhibitors for cancer therapy

Y Fang, C Yang, Z Yu, X Li, Q Mu, G Liao… - Acta Pharmaceutica Sinica …, 2021 - Elsevier
Natural products generally fall into the biologically relevant chemical space and always
possess novel biological activities, thus making them a rich source of lead compounds for …

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 …

Epidrug repurposing: discovering new faces of old acquaintances in cancer therapy

M Montalvo-Casimiro, R González-Barrios… - Frontiers in …, 2020 - frontiersin.org
Gene mutations are strongly associated with tumor progression and are well known in
cancer development. However, recently discovered epigenetic alterations have shown the …

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 …

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 …

Advances toward LSD1 inhibitors for cancer therapy

X Fu, P Zhang, B Yu - Future Medicinal Chemistry, 2017 - Taylor & Francis
LSD1 has become an important biologically validated epigenetic target for cancer therapy
since its identification in 2004. LSD1 mediates many cellular signaling pathways and is …

Comparison of orexin 1 and orexin 2 ligand binding modes using X-ray crystallography and computational analysis

M Rappas, AAE Ali, KA Bennett, JD Brown… - Journal of medicinal …, 2019 - ACS Publications
The orexin system, which consists of the two G protein-coupled receptors OX1 and OX2,
activated by the neuropeptides OX-A and OX-B, is firmly established as a key regulator of …

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 …