Targeting biomolecular condensation and protein aggregation against cancer

JL Silva, D Foguel, VF Ferreira, TCRG Vieira… - Chemical …, 2023 - ACS Publications
Biomolecular condensates, membrane-less entities arising from liquid–liquid phase
separation, hold dichotomous roles in health and disease. Alongside their physiological …

MDM2 inhibitors for cancer therapy: the past, present, and future

W Wang, N Albadari, Y Du, JF Fowler, HT Sang… - Pharmacological …, 2024 - Elsevier
Since its discovery over 35 years ago, MDM2 has emerged as an attractive target for the
development of cancer therapy. MDM2's activities extend from carcinogenesis to immunity to …

Cross-linking mass spectrometry (XL-MS): An emerging technology for interactomics and structural biology

C Yu, L Huang - Analytical chemistry, 2017 - pmc.ncbi.nlm.nih.gov
Protein-protein interactions are fundamental to the formation of intricate interaction networks
and the assembly of multisubunit protein complexes that represent the functional …

Chemistry and biology of multicomponent reactions

A Domling, W Wang, K Wang - Chemical reviews, 2012 - ACS Publications
Multicomponent reactions (MCRs) are one-pot reactions employing more than two starting
materials, for example, 3, 4,..., 7, where most of the atoms of the starting materials are …

MDM2, MDMX and p53 in oncogenesis and cancer therapy

M Wade, YC Li, GM Wahl - Nature Reviews Cancer, 2013 - nature.com
The MDM2 and MDMX (also known as HDMX and MDM4) proteins are deregulated in many
human cancers and exert their oncogenic activity predominantly by inhibiting the p53 tumour …

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 …

Clinical overview of MDM2/X-targeted therapies

A Burgess, KM Chia, S Haupt, D Thomas… - Frontiers in …, 2016 - frontiersin.org
MDM2 and MDMX are the primary negative regulators of p53, which under normal
conditions maintain low intracellular levels of p53 by targeting it to the proteasome for rapid …

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 …

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 roles of MDM2 and MDMX in cancer

O Karni-Schmidt, M Lokshin… - Annual Review of …, 2016 - annualreviews.org
For more than 25 years, MDM2 and its homolog MDMX (also known as MDM4) have been
shown to exert oncogenic activity. These two proteins are best understood as negative …