Manzamine A, an Orally Active β-Carboline Alkaloid with Antiviru, Antimalarial and Anticancer Activities
AManzamine A is an orally active β-carboline alkaloid effective against HSV-1, Cancer, and Malaria. For HSV-1， It is estimated that approximately 80% of the population worldwide are carriers of HSV-1 and approximately 40% suffer from recurrent infections. Unfortunately, this recurrent nature is a leading cause of corneal disease and...
STX-0119 is a Selective, Orally Active STAT3 Dimerization Inhibitor
STAT3 protein is a potential cytoplasmic transcription factor. Constitutive activation of signal transducer and activator of transcription 3 (STAT3) is related to the proliferation, survival, invasion, and angiogenesis of many human cancer cells. Specifically, it transmits signals of cytokines and growth factors from the cell membrane to the nucleus...
BNS-22 is a DNA Topoisomerase II Catalytic Inhibitor
Topoisomerases (DNA topoisomerases) are enzymes that catalyze changes in the topological state of DNA, regulating the overwinding or underwinding of DNA. Topoisomerases play essential roles in DNA replication, transcription, chromosome segregation, and recombination. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. All...
Linzagolix is a potent, non-Peptide, and Orally Active GnRH Antagonist
Uterine myomas and endometriosis are sex-hormone-dependent diseases. They affect up to 50-60% and 10-50% women of reproductive age, respectively. Endometriosis is an estrogen-dependent chronic inflammatory disease. The pathophysiology of this complex disease is multifactorial: in its pathogenesis, hormonal dysfunction, and proinflammatory microenvironment of eutopic and ectopic endometrium play a...
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...
IMT1 is a First-in-Class Specific and Noncompetitive Human POLRMT Inhibitor
Mitochondria provide cellular energy through its oxidative phosphorylation system, which needs to coordinate the expression of genes encoded by nuclear and mitochondrial genomes (mtDNA). Specifically, the transcription of mtDNA in circular mammals depends on a single mitochondrial RNA polymerase (POLRMT). Besides, three proteins are required for mitochondrial transcription initiation:...
TAS-119 is a Selective and Orally Active Aurora A Inhibitor
Aurora kinases represent a serine/threonine kinase family crucial for cell-cycle control. In particular, Aurora kinases are important and indispensable in multiple steps of mitotic progression. Specifically, Aurora kinase A acts primarily during the prophase of mitosis. Overexpression of Aurora A in HeLa cells attenuates the antiproliferative activity of Paclitaxel....