Topoisomerase 1B poisons: Over a half‐century of drug leads, clinical candidates, and serendipitous discoveries

MA Cinelli - Medicinal Research Reviews, 2019 - Wiley Online Library
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 inhibitors: Challenges, progress and the road ahead

A Talukdar, B Kundu, D Sarkar, S Goon… - European Journal of …, 2022 - Elsevier
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 …

DNA topoisomerases and their poisoning by anticancer and antibacterial drugs

Y Pommier, E Leo, HL Zhang, C Marchand - Chemistry & biology, 2010 - cell.com
DNA topoisomerases are the targets of important anticancer and antibacterial drugs.
Camptothecins and novel noncamptothecins in clinical development (indenoisoquinolines …

Discovery of new catalytic topoisomerase II inhibitors for anticancer therapeutics

VM Matias-Barrios, M Radaeva, Y Song… - Frontiers in …, 2021 - frontiersin.org
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-targeting chemotherapeutics: what's new?

SM Cuya, MA Bjornsti… - Cancer chemotherapy and …, 2017 - Springer
To resolve the topological problems that threaten the function and structural integrity of
nuclear and mitochondrial genomes and RNA molecules, human cells encode six different …

Targeting DNA topoisomerase II in cancer chemotherapy

JL Nitiss - Nature Reviews Cancer, 2009 - nature.com
Recent molecular studies have expanded the biological contexts in which topoisomerase II
(TOP2) has crucial functions, including DNA replication, transcription and chromosome …

Mechanisms of resistance to topoisomerase I-targeting drugs

ZA Rasheed, EH Rubin - Oncogene, 2003 - nature.com
DNA topoisomerases are a class of enzymes that alter the topology of DNA and are targets
of several anticancer drugs. Camptothecins (CPTs) are a relatively new family of compounds …

Recent advances in the development of dual topoisomerase I and II inhibitors as anticancer drugs

S Salerno, F Da Settimo, S Taliani… - Current medicinal …, 2010 - ingentaconnect.com
DNA topoisomerases (topos) are essential enzymes that regulate the topological state of
DNA during cellular processes such as replication, transcription, recombination, and …

Discovery and mechanistic study of tailor-made quinoline derivatives as topoisomerase 1 poison with potent anticancer activity

B Kundu, SK Das, S Paul Chowdhuri… - Journal of Medicinal …, 2019 - ACS Publications
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 …

ATP-bound topoisomerase II as a target for antitumor drugs

H Wang, Y Mao, N Zhou, T Hu, TS Hsieh… - Journal of Biological …, 2001 - ASBMB
Topoisomerase II (TOP2) poisons interfere with the breakage/reunion reaction of TOP2
resulting in DNA cleavage. In the current studies, we show that two different classes (ATP …