β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor
β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with DNA, which inhibits DNA replication,...
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...
Alda-1 is a potent ALDH2 Agonist
Aldehyde dehydrogenase 2 (ALDH2) is ubiquitously found in various tissues, including the heart, brain, and skeletal muscle, and highly expressed in the mitochondria. Many cellular functions show relations with ALDH2. They include detoxification of aldehydes, cell survival, cell proliferation, and apoptosis. The deficiency of ALDH2 causes the accumulation of...
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...
Trolox, an Analogue of Vitamin E, Possesses Antioxidant Effect
Oxidative stress reflects the imbalance between the systemic performance of reactive oxygen species (ROS) and the ability of biological systems to easily detoxify active intermediates or repair the resulting damage. Obviously, oxidative stress is considered to be related to the development of ADHD, cancer, Parkinson’s disease, Lafora disease, Alzheimer’s...
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...
Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis
Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...