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 …
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 …
cell (CSC)-mediated repopulation. We show that a fasting-mimicking diet (FMD) activates …
Discovery of a first-in-class EZH2 selective degrader
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 …
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
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 …
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 …
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 …
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 …
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 …
However, intrinsic or acquired unresponsiveness to immunotherapies does occur due to the …
[HTML][HTML] Targeting EZH2 in neuroblastoma
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 …
over 15% of all childhood cancer mortality. Risk stratification for children with neuroblastoma …