Category: Liver Cancer

Vatalanib (PTK787) is an Inhibitor of VEGFR2/KDR

Vascular endothelial growth factor receptor (VEGFR) is the receptor for VEGF. VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. VEGFRs consist of three subtypes, the fms-like tyrosine kinase Flt-1 (VEGFR1/Flt-1), the kinase domain region, also referred to as fetal liver kinase (VEGFR2/KDR/Flk-1), and Flt-4 (VEGFR3)....

ENMD-1198, an Orally Active Tubulin-Binding Agent, Reduces HIF-1α and STAT3 Activity

Hepatocellular carcinoma (HCC) is the fifth most cancer worldwide, with a continuously increasing incidence. HCC represents a hyper vascularized tumor and its progression is closely related to angiogenesis. Hepatocellular carcinoma overexpresses the vascular endothelial growth factor (VEGF). The transcription factor HIF-1α also plays a central role in HCC progression...

APG-1387, a Bivalent SMAC Mimetic, Induces Proteasomal Degradation of IAPs

Apoptosis protein inhibitors (IAP) are a class of functional and structural proteins, which are endogenous inhibitors of apoptosis. Specifically, inappropriate mutation or regulation will usually lead to cancer or other effects on cells. They include the Bcl-2 family, viral inhibitor crmA, and IAP’s. Besides, the most characteristic of IAAP...

PU02 is an Allosteric Antagonist of 5-HT3 Receptor

Cancer is a usual disease and a leading cause of death in the world. Therefore, developing new agents specifically targeting cancer cells has achieved more and more researches. As it is widely believed that cancer can be treated by inducing tumor cells to undergo senescence or apoptosis, screening for...

RJW100 is a Potent LRH-1 and SF-1 Agonist

Liver receptor homolog 1 (LRH-1, NR5A2) is a member of the nuclear receptor family. Specifically, LRH-1 plays a key role in regulating development, cholesterol transport, bile acid homeostasis, and steroid production. Besides, LRH-1 regulates hepatobiliary acid biosynthesis and cholesterol homeostasis and is the main controller of hepatobiliary. Therefore, the...

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...

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....