Tag: Antitumor

SBI-581 is An Orally Active Serine-Threonine Kinase TAO3 Inhibitor

TAO3 is a STE20-like kinase of the GCK subfamily. Specifically, TAO3 is overexpressed in many human cancers. Besides, it regulates the formation of invasive pseudopodia in melanoma, breast cancer, and bladder cancer. Both TAO3 and CBK1 are components of the RAM signal network, which regulate cell separation and polarization...

Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I

Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic produced by the actinomycete Saccharotrix aerocolonigenes with activity against several human tumor cell lines, including A549 (lung adenocarcinoma), HCT-116...

BrBzGCp2 is a Glyoxalase 1 Inhibitor, with Antitumor and Neuroprotective Activity

The glyoxalase system is a ubiquitous enzymatic network that plays important role in biological life. The glyoxalase system consists of glyoxalase 1 (GLO1), glyoxalase 2 (GLO2), and reduced glutathione (GSH). They perform an essential metabolic function in cells by detoxifying methylglyoxal (MG). GLO performs an essential metabolic function by...

MBQ-167 as a Dual Rac/Cdc42 Inhibitor in Metastatic Cancer

Rho GTPases participate in the regulation of cell migration, invasion, apoptosis, cell-to-cell and cell-to-extracellular matrix adhesions. The Rho GTPases Rac and Cdc42 potently induce actin polymerization. In addition, Cdc42 plays a critical role in cell polarity. Increasing studies have identified the effect of hyperactive Rac and Cdc42 on cancer...