Tag: Autophagy

GSK621 is a Specific AMPK Activator, Inducing Autophagy and Apoptosis

AMPK is an enzyme, which plays a role in cell energy homeostasis. It mainly activates glucose and fatty acid uptake and oxidation when the cell energy is low. Specifically, AMPK is a major regulator of cell metabolism, which can exert its carcinogenic or antitumor activities. Besides, the activation of...

THZ-P1-2 is a Selective PI5P4K Inhibitor

Phosphatidylinositol 5-phosphate (PI-5-P) is one of the seven phosphoinositides. They regulate a wide range of cellular functions. They localize in the nucleus, Golgi, endoplasmic reticulum, and at the plasma membrane. PI-5-P is an oxidative stress-induced regulator of AKT activation. The phosphorylation of the low abundance phosphoinositide PI-5-P at the...

MK-2206 is an Orally Active and Selective Allosteric Akt Inhibitor

Nasopharyngeal carcinoma (NPC) is a squamous cell carcinoma arising from the epithelium lining of the posterior nasopharynx. In a word, NPC causes very serious health problems in these areas. NPC is highly sensitive to radiation and chemotherapy. However, even with combined radiation and chemotherapy treatment, the prognosis for the...

GPP78 is a Nampt Inhibitor and an Autophagy Inducer

Nicotinamide phosphoribosyltransferase (NAMPT) is an enzyme that catalyzes the synthesis of nicotinamide mononucleotide (NMN) from nicotinamide (NM) and PRPP. Therefore, NAMPT plays an important role in the cyclic biosynthetic pathway of nicotinamide adenine dinucleotide (NAD). Especially, NAMPT acts as an extracellular proinflammatory cytokine, able to induce cellular expression of...

CA-5f is a Late-Stage Macroautophagy (Autophagy) Inhibitor for NSCLC Treatment

Currently, discovery of small-molecule modulators of autophagy has become a popular therapy for cancer treatment. A study from Lu Zhang has discovered and identified a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion, CA-5f. Autophagy plays essential roles in various normal cellular processes, including cell proliferation, ageing, and to...

MRT67307 Blocks mTOR-Dependent Autophagy by Inhibiting ULK1 Kinase

Yesterday, I introduced a dual IKKε/TBK1 inhibitor MRT67307. Studies have showed that MRT67307 plays a significant role in innate immunology. Not only this, a study from Katy J. Petherick drew a conclusion that MRT67307 blocked mTOR-dependent autophagy by inhibiting ULK1 kinase. ULK1, is believed to be specific for autophagy....