Epigenetics in cancer stem cells

TB Toh, JJ Lim, EKH Chow - Molecular cancer, 2017 - Springer
Compelling evidence have demonstrated that bulk tumors can arise from a unique subset of
cells commonly termed “cancer stem cells” that has been proposed to be a strong driving …

Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation: Miniperspective

S Xie, J Zhu, J Li, F Zhan, H Yao, J Xu… - Journal of Medicinal …, 2023 - ACS Publications
Targeted protein degradation (TPD) technologies have catalyzed a paradigm shift in
therapeutic strategies and offer innovative avenues for drug design. Hydrophobic tags …

Fasting-mimicking diet blocks triple-negative breast cancer and cancer stem cell escape

G Salvadori, F Zanardi, F Iannelli, R Lobefaro… - Cell metabolism, 2021 - cell.com
Metastatic tumors remain lethal due to primary/acquired resistance to therapy or cancer stem
cell (CSC)-mediated repopulation. We show that a fasting-mimicking diet (FMD) activates …

Discovery of a first-in-class EZH2 selective degrader

A Ma, E Stratikopoulos, KS Park, J Wei… - Nature chemical …, 2020 - nature.com
The enhancer of zeste homolog 2 (EZH2) is the main enzymatic subunit of the PRC2
complex, which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) to promote …

PALI1 promotes tumor growth through competitive recruitment of PRC2 to G9A-target chromatin for dual epigenetic silencing

K Fong, JC Zhao, X Lu, J Kim, A Piunti, A Shilatifard… - Molecular cell, 2022 - cell.com
PALI1 is a newly identified accessory protein of the Polycomb repressive complex 2 (PRC2)
that catalyzes H3K27 methylation. However, the roles of PALI1 in cancer are yet to be …

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 …

Discovery of precision targeting EZH2 degraders for triple-negative breast cancer

C Wang, X Chen, X Liu, D Lu, S Li, L Qu, F Yin… - European Journal of …, 2022 - Elsevier
EZH2 is usually overexpressed in TNBC and other tumors, which has a great influence on
the occurrence, development and prognosis of tumors. However, current EZH2 inhibitors …

Emerging role of G9a in cancer stemness and promises as a therapeutic target

JR Haebe, CJ Bergin, T Sandouka, YD Benoit - Oncogenesis, 2021 - nature.com
The histone methyltransferase G9a is well-documented for its implication in neoplastic
growth. However, recent investigations have demonstrated a key involvement of this …

EZH2 inhibition: a promising strategy to prevent cancer immune editing

N Kang, M Eccleston, PL Clermont, M Latarani… - …, 2020 - Taylor & Francis
Immunotherapies are revolutionizing the clinical management of a wide range of cancers.
However, intrinsic or acquired unresponsiveness to immunotherapies does occur due to the …

[HTML][HTML] Targeting EZH2 in neuroblastoma

J Gao, C Fosbrook, J Gibson, T Underwood… - Cancer Treatment …, 2023 - Elsevier
Neuroblastoma is one of the commonest extra-cranial pediatric tumors, and accounts for
over 15% of all childhood cancer mortality. Risk stratification for children with neuroblastoma …