Tag: Topoisomerase

TP3011 is a Potent Topoisomerase-1 Inhibitor with Anti-tumor Effect

Topoisomerases are proteins that cut the DNA backbone. Especially, topoisomerases let the cut ends twist past each other to a more relaxed configuration. Moreover, topoisomerases reseal the phosphodiester bonds in the backbone to again form an intact double helix. DNA topoisomerases I and II present in cells acts through...

NU1025 is a Potent PARP Inhibitor with Anti-Cancer and Neuroprotective Activity

Excessive glutamate release, Ca++ overload, free radical generation, poly (ADP-ribose) polymerase (PARP) overactivation are the main events of neuronal cell death in ischemic stroke. Besides, stroke is a third leading cause of death after heart diseases and cancer and a major cause of disabilities throughout the world. Moreover, excessive...

SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor

Research from Jeffrey R. Jackson, et al. discovered and identified an indolocarbazole inhibitor of human checkpoint Kinase (Chk1) SB-218078. SB-218078 is an ATP Competitive and Reversible Chk1 Inhibitor The regulation of cell cycle checkpoints is a critical determinant of the manner in which tumor cells in response to chemotherapies...

DRF-1042 is an Orally Active DNA topoisomerase I Inhibitor

Inhibitors of the enzyme topoisomerase I are cytotoxic for tumor cells because of their ability to cause DNA damage. Specifically, DNA Topoisomerase I (Top1) is one main cellular factor controlling topological homeostasis. Top1 activity can relax negative supercoils by cutting one of the DNA strands. This can create a...