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 …

Therapeutic strategies to activate p53

A Aguilar, S Wang - Pharmaceuticals, 2022 - mdpi.com
The p53 protein has appropriately been named the “guardian of the genome”. In almost all
human cancers, the powerful tumor suppressor function of p53 is compromised by a variety …

Chalcogen bonding in protein− ligand complexes: PDB survey and quantum mechanical calculations

K Kříž, J Fanfrlík, M Lepšík - ChemPhysChem, 2018 - Wiley Online Library
A chalcogen bond is a nonclassical noncovalent interaction which can stabilise small‐
molecule crystals as well as protein structures. Here, we systematically explore the …

Discovery of MK-4688: an Efficient Inhibitor of the HDM2–p53 Protein–Protein Interaction

MH Reutershan, MR Machacek… - Journal of Medicinal …, 2021 - ACS Publications
Identification of low-dose, low-molecular-weight, drug-like inhibitors of protein–protein
interactions (PPIs) is a challenging area of research. Despite the challenges, the therapeutic …

Recent small-molecule inhibitors of the p53–MDM2 protein–protein interaction

A Beloglazkina, N Zyk, A Majouga, E Beloglazkina - Molecules, 2020 - mdpi.com
This review presents the last decade of studies on the synthesis of various types of small-
molecule inhibitors of the p53–Mouse double minute 2 homolog (MDM2) protein–protein …

p53-Mdm2 interaction inhibitors as novel nongenotoxic anticancer agents

SK Nayak, GL Khatik, R Narang… - Current cancer drug …, 2018 - ingentaconnect.com
Background: Cancer is a major global health problem with high mortality rate. Most of the
clinically used anticancer agents induce apoptosis through genotoxic stress at various …

p53: An attractive therapeutic target for cancer

KR Patel, HD Patel - Current Medicinal Chemistry, 2020 - ingentaconnect.com
Cancer is a leading cause of death worldwide. It initiates when cell cycle regulatory genes
lose their function either by environmental and/or by internal factors. Tumor suppressor …

E3 ubiquitin ligase RNF148 functions as an oncogene in colorectal cancer by ubiquitination-mediated degradation of CHAC2

S Liu, L Zhuo, L Chen, Y He, X Chen, H Zhang… - …, 2024 - academic.oup.com
We previously reported that RNF148 was involved in the ubiquitination-mediated
degradation of CHAC2. However, its molecular mechanism was not determined. In this …

Spirocyclic degronimers for target protein degradation

AJ Phillips, CG Nasveschuk, JA Henderson, Y Liang… - 2017 - Google Patents
WO2017197036A1 - Spirocyclic degronimers for target protein degradation - Google Patents
WO2017197036A1 - Spirocyclic degronimers for target protein degradation - Google Patents …

Proteasomal degradation of Zn-dependent Hdacs: The E3-ligases implicated and the designed protacs that enable degradation

L Márquez-Cantudo, A Ramos, C Coderch… - Molecules, 2021 - mdpi.com
Protein degradation by the Ubiquitin-Proteasome System is one of the main mechanisms of
the regulation of cellular proteostasis, and the E3 ligases are the key effectors for the protein …