Tag: p53

GN25 is a Specific p53-Snail Binding Inhibitor with Antitumor Effects

P53, also known as Tumor protein P53, or transformation-related protein 53 (TRP53) is a regulatory protein that is often mutated in human cancers. Besides, p53 is the strongest tumor suppressor gene. In addition, p53 also induces cell death, and growth arrest and suppresses metastasis in response to various kinds...

CBL0137 is an Histone Chaperone FACT Inhibitor

Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...

MB710 is a Stabilizer of Oncogenic p53 Mutation Y220C

p53 acts as a tumor suppressor protein. Additionally, it plays s a pivotal role in several critical cellular processes, including cell-cycle regulation, DNA repair, and apoptosis. The p53 protein exerts its tumor suppressor function through complex and intricate regulatory processes. The tumor suppressor protein p53 plays a pivotal role...

NU9056 is a Selective Tip60 (KAT5) Histone Acetyltransferase Inhibitor

Histone acetylation and deacetylation are key events in the regulation of chromatin structure. Additionally, Histone acetyltransferases (HATs) can catalyze acetyl groups to the ε-amino terminus of lysine residues within histones. Acetylation results in an open chromatin structure by removing positive charges from histones. As a result, it induces protein...

MD-222 is a First-in-Class Highly Potent PROTAC Degrader of MDM2

PROTACs are heterobifunctional molecules that connect a POI ligand to an E3 ubiquitin ligase recruiting ligand with an optimal linker. Researchers reported the discovery of MD-222. MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53...

HLI373 is an Efficacious Hdm2 Inhibitor, with Antimalarial Activity

Hdm2 is an ubiquitin-protein ligase. Hdm2 suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. HLI373 is an efficacious Hdm2 inhibitor. HLI373 is effective in inducing apoptosis of several tumor cell lines that are sensitive to DNA-damaging agents. These results suggest that HLI373 could serve...

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...