Tag: NSCLC

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...

E7820 is an α2 Integrin Inhibitor with Anti-Tumor Activity

Vascular endothelial growth factor (VEGF) is a prime contributor to tumor angiogenesis. Most tumor cells produce high levels of VEGF and VEGF receptors associated with tumor endothelial cells. E7820 is an aromatic sulfonamide derivative and an Angiogenesis inhibitor. E7820 inhibits in vitro proliferation and tube formation of human umbilical...

BC-LI-0186 is a Selective Inhibitor of LeuRS and RagD Interaction

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). It competitively binds to the RagD interacting site of LRS (Kd=42.1 nM). At the same time, it has effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation, or the...

Mavelertinib is a Selective and Irreversible EGFR TKI

Mutant EGFRs are one of the major drivers of non-small-cell lung cancer (NSCLC). While reversible first-generation EGFR inhibitors are initially an effective treatment. However, a drug-resistant gatekeeper T790M mutation accounts for ∼50% of disease progression in patients with first-generation agents. Irreversible second-generation EGFR inhibitors are more potent against the...