Abstract Topoisomerase IB (Top1), a subcategory of DNA topoisomerase enzymes is
expressed much higher in several tumor cells. Therefore, modulating the activity of Top1 in …

To overcome chemical limitations of camptothecin (CPT), we report design, synthesis, and
validation of a quinoline-based novel class of topoisomerase 1 (Top1) inhibitors and …

Poison inhibitors of DNA topoisomerase II (TOP2) are clinically used drugs that cause
cancer cell death by inducing DNA damage, which mechanism of action is also associated …

DNA topoisomerase I (Top1) is over-expressed in tumour cells and is an important target in
cancer chemotherapy. It relaxes DNA torsional strain generated during DNA processing by …

Topoisomerases are DNA processing enzymes that relieve supercoiling (torsional strain) in
DNA, are necessary for normal cellular division, and act by nicking (and then religating) …

Topoisomerase I (TopoI), an essential enzyme, produces a DNA single strand break
allowing DNA relaxation for replication. The enzymatic mechanism involves sequential …

Drugs that inhibit or poison the function of topoisomerase (topo) enzymes are one of the
mainstays of cancer chemotherapy, and include some of the most widely used anticancer …

DNA topoisomerase II (TOP2) is a wellknown anticancer target. Its inhibitors are among the
most effective anticancer drugs currently in clinical use. TOP2-targeting agents fall into two …

Type II topoisomerases (Top2s) alter DNA topology via the formation of an enzyme–DNA
adduct termed cleavage complex, which harbors a transient double-strand break in one …

Camptothecin (CPT) and its derivatives target mammalian DNA topoisomerase I (top1) and
are among the most effective novel anticancer drugs. However, the activity of CPTs is limited …