Category: Glioma

Aderbasib is a Highly Potent and Orally Active Inhibitor of ADAM10 and ADAM17

ADAMs (a disintegrin and metalloproteinases), originally also known as MDC proteins (metalloproteinase/disintegrin/cysteine-rich). And ADAMs belong to the Metzincins superfamily of metalloproteases. Recently, studies have found ADAM genes exist in animals, choanoflagellates, fungi and some groups of green algae. Importantly, ADAMs mediates proteolytic ectodomain release. And the ectodomain shedding is...

Nimotuzumab is a Humanized IgG1 Monoclonal Antibody Targeting EGFR

The epidermal growth factor receptor (EGFR) is a transmembrane protein. The dimerization of EGFR stimulates the activity of intracellular protein tyrosine kinase. Therefore, several tyrosine (y) residues in the C-terminal domain of EGFR undergo autophosphorylation. These include y992, y1045, y1068, y1148, and y1173, as shown in the adjacent chart....

Vorasidenib (AG-881) is an Orally Available, Brain Penetrant and dual mIDH1/2 Inhibitor

Isocitrate dehydrogenases 1 and 2 (IDH1/2) are homodimeric enzymes. They catalyze the conversion of isocitrate to α-ketoglutarate (α-KG) in the tricarboxylic acid cycle. However, mutant IDH1/2 (mIDH1/2) reduces α-KG to the oncometabolite 2-hydroxyglutarate (2-HG). Inhibition of the mutant IDH (mIDH) protein represents a targeted approach to cancer treatment for...

Lonafarnib is an Orally Active FPTase Inhibitor

Farnesyl transferase (FTase) is a zinc-dependent enzyme, which coordinates a zinc cation on its β subunit at the lip of the active site. FTase has two subunits: a 48kDa α-subunit and a 46kDa β-subunit. And it adds a 15-carbon isoprenoid called a farnesyl group to proteins bearing a CaaX...

A-674563 is an Orally Active and Selective Akt1 Inhibitor

Akt1 belongs to the Akt subfamily of serine/threonine kinases, which contains the SH2 (SRC homologous 2-like) domain. Specifically, Akt kinase is the central node of the signal transduction pathway, which is important for cell transformation and tumor progression. Besides, Akt is a key mediator of growth factor-induced neuronal survival...

BIM-23190 is a Selective SSTR2 and SSTR5 Agonist

Somatostatin (SST) is a peptide hormone, which can regulate the endocrine system. Specifically, Somatostatin affects neurotransmission and cell proliferation by interacting with G protein-coupled somatostatin receptors and inhibiting multiple releases. Besides, Somatostatin inhibits insulin and glucagon secretion. Moreover, Somatostatin is produced by neuroendocrine neurons in the hypothalamic extraperitoneal nucleus....

AKI603 is an Aurora Kinase A Inhibitor with Anti-tumor Activity

Chemoresistance is a major cause of cancer treatment failure. Tumor-initiating cells (TIC) have attracted a considerable amount of attention due to their role in chemoresistance and tumor recurrence. The inhibition of AurA kinase by AKI603 abrogates the epirubicin-induced enrichment of TICs.In this study, researchers evaluated the small molecule Aurora...