Tag: Topoisomerase

Daunorubicin is a Topoisomerase II Inhibitor with potent Antineoplastic Activities

Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation...

SN-38 (NK012) is an Active Metabolite of the Topoisomerase I Inhibitor Irinotecan

DNA topoisomerase I (Top1) is a DNA unwinding protein and the specific target of the camptothecin class of chemotherapeutic drugs. Top1 binds supercoiled DNA, nicks a DNA strand allowing its rotation around the intact strand, and then relegates the DNA. Camptothecins bind and stabilize the Top1-DNA cleavage complexes, thus...

CRT0044876 is a Potent and Selective APE1 Inhibitor

The base excision repair (BER) pathway is essential for the removal of DNA bases damaged by alkylation or oxidation. This pathway also handles a variety of other lesions including deaminated bases and DNA single-strand breaks. A key step in BER is the processing of an apurinic/apyrimidinic (AP) site intermediate...

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...