CMLD-2 is Inhibits HuR and Induces Apoptosis
Hu antigen R (HuR) is an RNA binding protein. Specifically, Its overexpression in human cancer is associated with aggressive disease, drug resistance, and poor prognosis. HuR is highly abundant in many types of cancer and promotes tumorigenesis through cancer-related mRNA interactions. Besides, HuR has related to the regulation of...
Afatinib is an Irreversible and Orally Active EGFR Family Inhibitor
Lung cancer continues to be the leading cause of cancer-related mortality. Members of the ERBB receptor tyrosine kinase family include EGFR, HER2, HER3, and HER4. They present an attractive option for targeted therapy in patients with NSCLC, due to observed patterns of oncogenic mutation of EGFR and HER2. In addition, esophageal...
CTPI-2 is a Mitochondrial Citrate Carrier SLC25A1 Inhibitor
Nonalcoholic fatty liver disease (NAFLD) and inflammatory steatohepatitis (NASH) comprise a series of manifestations that span from reversible hepatic steatosis to progressive necroinflammatory and fibrotic disease. There exists a clear association between NASH with obesity, diabetes, and metabolic syndrome. Slc25a1 is a mitochondrial citrate carrier, which belongs to a...
EMI56 is a Superior Mutant EGFR Inhibitor
Receptor Tyrosine Kinases (RTKs) play critical roles in embryogenesis, normal physiology, and several diseases. Epidermal growth factor receptor (EGFR) is a transmembrane protein with cytoplasmic kinase activity that transduces important growth factor signaling from the extracellular milieu to the cell. Furthermore, EGFR common double mutations include 19Del, L858R, and...
VZ185 is a Selective Dual BRD7/9 PROTAC Degrader
Targeted protein degradation is an emerging strategy to use small molecules to knock down a protein by hijacking the ubiquitin-proteasome system. PROTACs are bifunctional degrader molecules. They compose a ligand for the target protein and a ligand for E3 ligase recruitment, connected by a linker. An attractive feature of...
BI-3663 is a Highly Selective PTK2/FAK PROTAC
Focal adhesion tyrosine kinase (PTK2) is a cytoplasmic protein tyrosine kinase. PTK2 plays an important role in adhesion, spreading, motility, invasion, metastasis, survival, angiogenesis, epithelial to mesenchymal transition, cancer stem cells, and the tumor microenvironment. Overexpression and activation of PTK2 connect with several human malignant diseases, including colorectal, ovarian,...
Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor
Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...