Prospects of Topoisomerase Inhibitors as Promising Anti-Cancer Agents
Topoisomerases are very important enzymes that regulate DNA topology and are vital for biological actions like DNA replication, transcription, and repair. The emergence and spread of cancer has been intimately associated with topoisomerase dysregulation.
Prasanna Anjaneyulu Yakkala +3 more
doaj +4 more sources
Mechanisms regulating resistance to inhibitors of topoisomerase II [PDF]
Inhibitors of topoisomerase II (topo II) are clinically effective in the management of hematological malignancies and solid tumors. The efficacy of anti-tumor drugs targeting topo II is often limited by resistance and studies with in vitro cell culture ...
Ram N. Ganapathi, Mahrukh K. Ganapathi
doaj +7 more sources
A Mini Review of Novel Topoisomerase II Inhibitors as Future Anticancer Agents [PDF]
Several reviews of inhibitors of topoisomerase II have been published, covering research before 2018. Therefore, this review is focused primarily on more recent publications with relevant points from the earlier literature.
Toluwase Hezekiah Fatoki
exaly +3 more sources
The Implication of Topoisomerase II Inhibitors in Synthetic Lethality for Cancer Therapy [PDF]
DNA topoisomerase II (Top2) is essential for all eukaryotic cells in the regulation of DNA topology through the generation of temporary double-strand breaks.
Victor M. Matias-Barrios, Xuesen Dong
doaj +2 more sources
Hyperthermia, thermotolerance and topoisomerase II inhibitors [PDF]
The cytoxicity of both intercalating (m-AMSA) and non-intercalating (VP16, VM26) topoisomerase II-targeting drugs is thought to occur via trapping DNA topoisomerase II on DNA in the form of cleavable complexes. First, analysis of cleavable complexes (detected as DNA double-strand breaks) by pulsed-field gel electrophoresis confirmed the correlation ...
HH Kampinga +2 more
core +5 more sources
In Silico Evaluation of Some Computer-Designed Fluoroquinolone–Glutamic Acid Hybrids as Potential Topoisomerase II Inhibitors with Anti-Cancer Effect [PDF]
Background/Objectives: Fluoroquinolones (FQs) are topoisomerase II inhibitors with antibacterial activity, repositioned recently as anti-cancer agents. Glutamic acid (GLA) is an amino acid that affects human metabolism.
Octavia-Laura Oancea +4 more
doaj +2 more sources
Discovery of New Catalytic Topoisomerase II Inhibitors for Anticancer Therapeutics [PDF]
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 with serious side effects such as secondary malignancy and cardiotoxicity.
Victor M. Matias-Barrios +14 more
doaj +2 more sources
Topoisomerase II as a Novel Antiviral Target against Panarenaviral Diseases
Although many arenaviruses cause severe diseases with high fatality rates each year, treatment options are limited to off-label use of ribavirin, and a Food and Drug Administration (FDA)-approved vaccine is not available.
Tosin Oladipo Afowowe +4 more
doaj +3 more sources
Phosphodiesterase Type 5 (PDE5) Inhibitors Sensitize Topoisomerase II Inhibitors in Killing Prostate Cancer Through PDE5-Independent Impairment of HR and NHEJ DNA Repair Systems [PDF]
Human castration-resistant prostate cancer (CRPC) is a significant target of clinical research. The use of DNA-damaging agents has a long history in cancer chemotherapy but is limited by their toxicities.
Jo-Fan Chang +10 more
doaj +2 more sources
Tetrahydropyrido[4,3-d]pyrimidines as a new active scaffold for human topoisomerase II inhibitors [PDF]
Human topoisomerase II (topoII) is a well-known and validated target for cancer treatment. We previously reported a first set of 6-amino-tetrahydroquinazoline derivatives as novel human topoII inhibitors.
Nicoletta Brindani +9 more
doaj +2 more sources

