Tag: Autophagy

5-Azacytidine, a Nucleoside Analogue of Cytidine, Inhibits DNA Methylation

In the mammalian genome, DNA methylation is an epigenetic mechanism involving the transfer of a methyl group onto the C5 position of the cytosine to form 5-methylcytosine. DNA methylation regulates gene expression by recruiting proteins involved in gene repression or by inhibiting the binding of transcription factor(s) to DNA....

Chelerythrine is a Potent Protein kinase C Inhibitor

Chelerythrine is a natural benzo[c]phenanthridine alkaloid. It extracts from a number of plant species, such as Chelidonium majus, Macleaya cordata, Sanguinaria canadensis, etc. This compound exerts a wide spectrum of biological activities, including anti-cancer, anti-diabetes, anti-fungus, as well as a protective effect against the ethanol-induced gastric ulcer and the...

Deguelin, a Naturally Occurring Rotenoid, Acts as a Chemopreventive Agent

Head and neck squamous cell carcinoma (HNSCC) represents more than 5% of all cancers each year. In addition, breast cancer is a heterogeneous group of diseases. Approximately 60-70% of breast cancers express estrogen receptors (ER) and/or progesterone receptors (PR). About 20-30% of breast cancers have amplified levels of the...

ABT-737 is a Selective and BH3 Mimetic Bcl-2, Bcl-xL and Bcl-w Inhibitor

Bcl-2 protein family is a key regulator of apoptosis and a marker of B-cell lymphoma. Importantly, apoptosis is an important physiological process of selective cell clearance, involving a variety of biological events. Particularly, the Bcl-2 family is the most characteristic protein family involved in regulating apoptotic cell death. It...

Spautin-1 is a Specific and Potent Autophagy Inhibitor

Autophagy refers to the natural and conservative degradation of cells through lysosome dependent regulation mechanism. Specifically, it allows the orderly degradation and recovery of cellular components. At present, there are four forms of autophagy: macroautophagy, microautophagy, chaperone-mediated autophagy (CMA), and coprophagy. The catabolic process of macroautophagy is evolutionarily conserved...

Sapanisertib is an Orally Active and ATP-Dependent mTOR Inhibitor

Acute myelogenous leukemia (AML) is a heterogeneous disease. It often relapses after standard chemotherapy or proves refractory to available treatments. Therefore, It needs novel therapies for AML. In AML, many signaling pathways are abnormally activated and lead to uncontrolled proliferation/survival of immature myeloid progenitors. The 50% to 80% of...

GSK2606414 is an Orally Available PERK Inhibitor

PERK (Protein kinase R (PKR)-like endoplasmic reticulum kinase) is a type I endoplasmic reticulum transmembrane protein. Generally, PERK contains a stress-sensing domain facing the endoplasmic reticulum lumen and a cytosolic kinase domain. Interestingly, PERK is a major component of the unfolded protein response (UPR), which promotes the adaptation of...