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 …

The paradigm of drug resistance in cancer: an epigenetic perspective

S Adhikari, A Bhattacharya, S Adhikary… - Bioscience …, 2022 - portlandpress.com
Innate and acquired resistance towards the conventional therapeutic regimen imposes a
significant challenge for the successful management of cancer for decades. In patients with …

Proteomic characterization of post-translational modifications in drug discovery

L Zhai, K Chen, B Hao, M Tan - Acta Pharmacologica Sinica, 2022 - nature.com
Protein post-translational modifications (PTMs), which are usually enzymatically catalyzed,
are major regulators of protein activity and involved in almost all celluar processes …

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 …

Lysine-specific demethylase 1 promises to be a novel target in cancer drug resistance: therapeutic implications

FF Yang, XL Xu, T Hu, JQ Liu, JZ Zhou… - Journal of Medicinal …, 2023 - ACS Publications
Chemotherapy, targeted therapy, and immunotherapy are effective against most tumors, but
drug resistance remains a barrier to successful treatment. Lysine-specific demethylase 1 …

Regulating methylation at H3K27: a trick or treat for cancer cell plasticity

P Das, JH Taube - Cancers, 2020 - mdpi.com
Simple Summary Regulation of gene expression is important for appropriate cell
development but can also lead to inappropriate cell transformation resulting in cancer …

X-and Y-linked chromatin-modifying genes as regulators of sex-specific cancer incidence and prognosis

R Tricarico, E Nicolas, MJ Hall, EA Golemis - Clinical Cancer Research, 2020 - AACR
Biological sex profoundly conditions organismal development and physiology, imposing
wide-ranging effects on cell signaling, metabolism, and immune response. These effects …

Understanding the mechanisms by which epigenetic modifiers avert therapy resistance in cancer

A Quagliano, A Gopalakrishnapillai, SP Barwe - Frontiers in oncology, 2020 - frontiersin.org
The development of resistance to anti-cancer therapeutics remains one of the core issues
preventing the improvement of survival rates in cancer. Therapy resistance can arise in a …

Targeting histone modifications in breast cancer: a precise weapon on the way

W Li, H Wu, S Sui, Q Wang, S Xu… - Frontiers in cell and …, 2021 - frontiersin.org
Histone modifications (HMs) contribute to maintaining genomic stability, transcription, DNA
repair, and modulating chromatin in cancer cells. Furthermore, HMs are dynamic and …

Exploring the potential of histone demethylase inhibition in multi-therapeutic approaches for cancer treatment

D Li, H Liang, Y Wei, H Xiao, X Peng, W Pan - European Journal of …, 2023 - Elsevier
Histone demethylases play a critical role in gene transcription regulation and have been
implicated in cancer. Numerous reports have highlighted the overexpression of histone …