Tag: Metastasis

ZINC69391 is a Specific Rac1 Inhibitor and Apoptosis Inducer

Rho-GTPases are molecular switches that cycle between an inactive GDP-bound form and an active GTP-bound form. Guanine nucleotide exchange factors (GEFs) catalyze nucleotide exchange and mediate activation in this cycle, While GTPase-activating proteins (GAPs) stimulate GTP hydrolysis and inactivate the GTPase. Only the active GTP-bound state binds to downstream...

ZLDI-8, an ADAM-17 and Notch Inhibitor, Enhances Chemotherapeutic Effects

ADAM metallopeptidase domain 17 (ADAM17) is an enzyme that belongs to the ADAM protein family of metalloproteases. ADAM17 plays a prominent role in the Notch signaling pathway. In this study, researchers demonstrated the discovery of ZLDI-8. ZLDI-8 is a novel inhibitor for Notch activating/cleaving enzyme ADAM-17. In particular, ZLDI-8...

6RK73 is a Covalent Irreversible and Specific UCHL1 Inhibitor

Approximately 90% of breast cancer-related deaths are due to metastasis. During the metastasis process, epithelial-mesenchymal transition (EMT) plays an important role. The secreted cytokine transforming growth factor-β (TGFβ) can induce it. Breast cancer has multiple subtypes with distinct metastatic potential based on genetic and clinical features. The most aggressive...

PI-103 is a Potent PI3K and mTOR Inhibitor

The phosphatidylinositide 3-kinase family possesses 15 members. those members consist of four distinct classes as a basis on their structure and biological properties. As we all know, this highly conserved family of enzymes involves various aspects of cellular homeostasis and exists a decline in a number of pathophysiologic conditions....

CWP232228 is a Highly Potent and Selective Wnt/β-catenin Inhibitor

Conventional chemotherapy and radiation induce more and more breast cancer stem cells (BCSC) resistance. In recent years, increasing studies have suggested that the dysregulation of Wnt/β-catenin signaling occurs in breast cancer. A study from Gyu-Beom Jang, the researchers showed that the level of Wnt/β-catenin signaling in BCSC is relatively...

Alpelisib is a Selective and Orally Active PI3Kα Inhibitor for Metastatic Breast Cancer

Phosphatidylinositol-3-kinases (PI3Ks) are a family of important lipid kinases. PI3Ks are important in controlling the signaling pathways involved in cell proliferation, motility, cell death, and cell invasion. Moreover, PI3Ks control and deliver cellular signals in the PI3K/Akt/mTOR pathway by phosphorylating phosphatidylinositol 4,5-bisphosphate (PIP2) to phosphatidylinositol 3,4,5-trisphosphate (PIP3) on the...