ARN24139 is a TopoII Inhibitor with Promising Antiproliferative Activity
Topoisomerase II is a ubiquitous enzyme in all branches of life that alters DNA supercoils and breaks double-stranded DNA fragments during processes such as replication and transcription. Eukaryotic Topoisomerase II functions as a homodimer and requires ATP and divalent metal ions for overall catalytic activity. It interconverts different topologies...
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...