Targeting epigenetic regulators to overcome drug resistance in cancers

N Wang, T Ma, B Yu - Signal transduction and targeted therapy, 2023 - nature.com
Drug resistance is mainly responsible for cancer recurrence and poor prognosis. Epigenetic
regulation is a heritable change in gene expressions independent of nucleotide sequence …

Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

BRD4-directed super-enhancer organization of transcription repression programs links to chemotherapeutic efficacy in breast cancer

B Liu, X Liu, L Han, X Chen, X Wu… - Proceedings of the …, 2022 - National Acad Sciences
BRD4 is well known for its role in super-enhancer organization and transcription activation
of several prominent oncogenes including c-MYC and BCL2. As such, BRD4 inhibitors are …

Epithelial-mesenchymal transition (EMT) as a therapeutic target

S Jonckheere, J Adams, D De Groote… - Cells Tissues …, 2022 - karger.com
Metastasis is the spread of cancer cells from the primary tumour to distant sites and organs
throughout the body. It is the primary cause of cancer morbidity and mortality, and is …

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 …

YAP/TAZ drives cell proliferation and tumour growth via a polyamine–eIF5A hypusination–LSD1 axis

H Li, BK Wu, M Kanchwala, J Cai, L Wang, C Xing… - Nature cell …, 2022 - nature.com
Metabolic reprogramming is central to oncogene-induced tumorigenesis by providing the
necessary building blocks and energy sources, but how oncogenic signalling controls …

Discovery of CC-90011: a potent and selective reversible inhibitor of lysine specific demethylase 1 (LSD1)

T Kanouni, C Severin, RW Cho, NYY Yuen… - Journal of Medicinal …, 2020 - ACS Publications
Histone demethylase LSDl (KDMlA) belongs to the flavin adenine dinucleotide (FAD)
dependent family of monoamine oxidases and is vital in regulation of mammalian biology …

Expanding the role of the histone lysine-specific demethylase LSD1 in cancer

B Majello, F Gorini, CD Saccà, S Amente - Cancers, 2019 - mdpi.com
Studies of alterations in histone methylation in cancer have led to the identification of histone
methyltransferases and demethylases as novel targets for therapy. Lysine-specific …

Targeting epigenetics: A novel promise for Alzheimer's disease treatment

D Jeremic, L Jiménez-Díaz, JD Navarro-López - Ageing Research Reviews, 2023 - Elsevier
So far, the search for a cure for Alzheimer Disease (AD) has been unsuccessful. The only
approved drugs attenuate some symptoms, but do not halt the progress of this disease …

[HTML][HTML] UM171 preserves epigenetic marks that are reduced in ex vivo culture of human HSCs via potentiation of the CLR3-KBTBD4 complex

J Chagraoui, S Girard, JF Spinella, L Simon, E Bonneil… - Cell Stem Cell, 2021 - cell.com
Human hematopoietic stem cells (HSCs) exhibit attrition of their self-renewal capacity when
cultured ex vivo, a process that is partially reversed upon treatment with epigenetic …