JCN037 is a Non-Covalent and Brain-Penetrant EGFR Inhibitor
The epidermal growth factor receptor (EGFR) is a transmembrane protein that is a receptor for members of the EGF family of extracellular protein ligands. In many cancer types, mutations affecting EGFR expression or activity could result in cancer. Specifically, EGFR gene changes occurred in nearly 60% of glioblastoma tumors....
TED-347 is an Irreversible and Covalent YAP-TEAD Protein-Protein Interaction Inhibitor
Yap1, also known as Yap, is a protein that acts as a transcription regulator by activating the transcription of genes involved in cell proliferation and inhibiting apoptosis. Specifically, Yap1 is inhibited in the hippopotamus signaling pathway, which can control organ size and inhibit tumors. Besides, hippopotamus signaling regulates Yap1...
AMG 511 is an Orally Active pan-PI3K Inhibitor
The PI3K signaling network has a central role in several cellular processes critical to the initiation and progression of cancer, including growth, survival, and metabolism. The PI3K family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger that plays a critical role in important cellular functions such as...
TCH-165, a Proteasome Assembly Modulator, Regulates the Dynamic Equilibrium between the 20S and 26S Proteasome Complexes
Intrinsically disordered proteins (IDPs) involves a number of multiple regulatory and signaling events. In addition, the accumulation of IDPs results in some harmful signals happening in the pathogenesis of many human diseases. The proteasome contains different include active complexes (such as the 26S proteasome) and a weakly active complex: the...
M8891 is an Orally Active and Brain Penetrant MetAP-2 Inhibitor
Removal of N-terminal methionine by methionine aminopeptidases (MetAP) is a crucial step in the maturation of proteins during protein biosynthesis. Besides, MetAP-2 is one of the two cytoplasmic methionine aminopeptidases expressed in mammalian cells. Moreover, MetAP-2 acts as a target of the highly potent and irreversible inhibitor fumagillin to...
Gboxin is an Oxidative Phosphorylation Inhibitor That Targets Glioblastoma
According to the World Health Organization (WHO), Glioblastoma is the most common primary brain neoplasm. It comprises 15% of all intracranial neoplasms and 60-75% of astrocytic tumors. Unfortunately, Glioblastoma is the most aggressive and prevalent primary malignant brain tumor of the central nervous system. Glioblastoma derives specifically from the...
RIPGBM is a Selective Inducer of Apoptosis in Glioblastoma Multiforme Cancer Stem Cells
Glioblastoma multiforme is the most prevalent and aggressive form of primary brain cancer. Glioblastoma multiforme is the most hostile type of brain cancer. Its aggressiveness is due to increased invasion, migration, proliferation, angiogenesis, and a decreased apoptosis. Crucially, a sub-population of multi-potent cells term glioblastoma multiforme cancer stem cells...