Tag: Autophagy

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...

Birinapant (TL32711), a Bivalent Smac Mimetic, is an Antagonist for XIAP and cIAP1

XIAP is a protein that prevents apoptosis. XIAP is a member of apoptosis protein family (IAP) inhibitors. Specifically, IAP blocks cell death in vitro and in vivo by inhibiting different caspases. The caspase inhibitory activity of XIAP is negatively regulated by at least two XIAP interacting proteins XAF1 and...

Wortmannin (SL-2052) is an Orally Active, Selective and Irreversible PI3K Inhibitor

Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ. There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K,...