AZD1390 is a Highly Selective, Orally Active and Brain-Penetrant ATM Inhibitor
Glioblastoma multiforme (GBM) is a lethal form of brain tumor arising from malignant glial cells. this disease affects 2 to 3 per 100,000 adults per year and accounts for 52% of all primary brain tumors. ATM plays a central role in the detection, signaling, and repair of DNA double-strand...
NAZ2329 is an Allosteric Inhibitor of R5 RPTP Subfamily and PTPRZ/PTPRG
The R5 subfamily of receptor protein tyrosine phosphatases (RPTPs) includes PTPRZ and PTPRG. Specifically, PTPRZ1 is a member of the receptor tyrosine phosphatase family. Besides, PTPRZ1 encodes a one-way type I membrane protein with two cytoplasmic tyrosine-protein phosphatase domains, α-carbonic anhydrase domain, and fibronectin III domain. There is a...
PINT87aa, a Potential Tumor-Suppressive Peptide, Directly Interacts with the PAF1 Complex
Circular RNAs (circRNAs) are a large class of transcripts in the mammalian genome. CircRNAs are inherently resistant to exonuclease activity (resulting in higher stability than linear RNAs) and often show tissue- or developmental stage-specific expression. It suggests that they possess important biological functions. To date, circRNAs can act as microRNA...
RapaLink-1, a Third-Generation Bivalent mTOR Inhibitor, Combines Rapamycin with MLN0128
Glioblastoma (GBM), the most common primary brain tumor, represents one of the most aggressive cancers. The signaling from PI3K and AKT to mTOR is commonly dysregulated in GBM. But, blockade of these upstream targets minimally affects mTOR activity in glioma. Allosteric mTOR inhibitors, such as rapamycin, incompletely block mTORC1...
AMG-458 is a Selective and Orally Bioavailable c-Met Inhibitor
C-met is a protein encoded by a met gene in humans, which has tyrosine kinase activity. Specifically, Met is an essential one-way tyrosine kinase receptor for embryonic development, organogenesis, and wound healing. Besides, C-met is a receptor tyrosine kinase that can be activated by its ligand, hepatocyte growth factor/dispersion...
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...