Undruggable proteins are a class of proteins that are often characterized by large, complex
structures or functions that are difficult to interfere with using conventional drug design …

The γ-lactam moiety is present in a large number of natural and non-natural biologically
active compounds. The range of biological activities covered by these compounds is very …

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 …

The p53 tumor suppressor is a key transcription factor regulating cellular pathways such as
DNA repair, cell cycle, apoptosis, angiogenesis, and senescence. It acts as an important …

The emergence and convergence of cancer genomics, targeted therapies, and network
oncology have significantly expanded the landscape of protein–protein interaction (PPI) …

Targeting protein–protein interactions (PPIs) has emerged as a viable approach in modern
drug discovery. However, the identification of small molecules enabling us to effectively …

Proteasome-mediated degradation is a common mechanism by which cells renew their
intracellular proteins and maintain protein homeostasis. In this process, the E3 ubiquitin …

G protein–coupled receptors (GPCRs) play critical roles in regulating processes such as
cellular homeostasis, responses to stimuli, and cell signaling. Accordingly, GPCRs have …

MDM4 is a homologue of MDM2, serving cooperatively as the negative regulator of tumor
suppressor p53. Under the shadow of MDM2 inhibitors, limited efforts had been put into the …

Abstract Blocking the MDM2/X–P53 protein–protein interaction has been widely recognized
as an attractive therapeutic strategy for the treatment of cancers. Numerous small-molecule …