Targeting transcription factors in cancer—from undruggable to reality

JH Bushweller - Nature Reviews Cancer, 2019 - nature.com
Mutated or dysregulated transcription factors represent a unique class of drug targets that
mediate aberrant gene expression, including blockade of differentiation and cell death gene …

Sex differences in cancer mechanisms

JB Rubin, JS Lagas, L Broestl, J Sponagel… - Biology of sex …, 2020 - Springer
We now know that cancer is many different diseases, with great variation even within a
single histological subtype. With the current emphasis on developing personalized …

Small-molecule inhibitors of the MDM2–p53 protein–protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment: miniperspective

Y Zhao, A Aguilar, D Bernard… - Journal of medicinal …, 2015 - ACS Publications
Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–
protein interaction has been pursued as a new cancer therapeutic strategy. In recent years …

Discovery of RG7388, a potent and selective p53–MDM2 inhibitor in clinical development

Q Ding, Z Zhang, JJ Liu, N Jiang, J Zhang… - Journal of medicinal …, 2013 - ACS Publications
Restoration of p53 activity by inhibition of the p53–MDM2 interaction has been considered
an attractive approach for cancer treatment. However, the hydrophobic protein–protein …

Targeting the MDM2–p53 protein–protein interaction for new cancer therapy: progress and challenges

S Wang, Y Zhao, A Aguilar… - Cold Spring …, 2017 - perspectivesinmedicine.cshlp.org
MDM2 is a primary cellular inhibitor of p53. It inhibits p53 function by multiple mechanisms,
each of which, however, is mediated by their direct interaction. It has been proposed that …

SAR405838: an optimized inhibitor of MDM2–p53 interaction that induces complete and durable tumor regression

S Wang, W Sun, Y Zhao, D McEachern, I Meaux… - Cancer research, 2014 - AACR
Blocking the oncoprotein murine double minute 2 (MDM2)–p53 protein–protein interaction
has long been considered to offer a broad cancer therapeutic strategy, despite the potential …

Discovery of RG7112: a small-molecule MDM2 inhibitor in clinical development

B Vu, P Wovkulich, G Pizzolato, A Lovey… - ACS medicinal …, 2013 - ACS Publications
The p53 tumor suppressor is a potent transcription factor that plays a key role in the
regulation of cellular responses to stress. It is controlled by its negative regulator MDM2 …

Small-molecule MDM2 inhibitors in clinical trials for cancer therapy

S Wang, FE Chen - European journal of medicinal chemistry, 2022 - Elsevier
Disruption of the MDM2-p53 protein-protein interaction by small-molecule inhibitors has
been highly pursued by many academic laboratories and pharmaceutical companies as a …

The genetics of the p53 pathway, apoptosis and cancer therapy

A Vazquez, EE Bond, AJ Levine, GL Bond - Nature reviews Drug …, 2008 - nature.com
The p53 pathway has been shown to mediate cellular stress responses; p53 can initiate
DNA repair, cell-cycle arrest, senescence and, importantly, apoptosis. These responses …

Long non-coding RNA PVT1 interacts with MYC and its downstream molecules to synergistically promote tumorigenesis

K Jin, S Wang, Y Zhang, M Xia, Y Mo, X Li, G Li… - Cellular and Molecular …, 2019 - Springer
Numerous studies have shown that non-coding RNAs play crucial roles in the development
and progression of various tumor cells. Plasmacytoma variant translocation 1 (PVT1) mainly …