Organometallic iridium(III) anticancer complexes with new mechanisms of action: NCI-60 screening, mitochondrial targeting, and apoptosis [PDF]
Platinum complexes related to cisplatin, cis-[PtCl2(NH3)2], are successful anticancer drugs; however, other transition metal complexes offer potential for combating cisplatin resistance, decreasing side effects, and widening the spectrum of activity ...
Bailey H. H. +67 more
core +1 more source
Heterocyclic bibenzimidazole derivatives as topoisomerase I inhibitors [PDF]
A series of 2'-heterocyclic derivatives of 5-phenyl-2,5'-1H-bibenzimidazoles were evaluated for topoisomerase I poisoning activity and cytotoxicity. Topo I poisoning activity was associated with 2'-derivatives that possessed a hydrogen atom capable of hydrogen bond formation, suggesting that the interatomic distances between such hydrogen atoms and the
Jin, S. +6 more
openaire +2 more sources
Hybrid topoisomerase I and HDAC inhibitors as dual action anticancer agents. [PDF]
Recent studies have shown that HDAC inhibitors act synergistically with camptothecin derivatives in combination therapies. To exploit this synergy, new hybrid molecules targeting simultaneously topoisomerase I and HDAC were designed.
Raffaella Cincinelli +12 more
doaj +1 more source
Independence from kinetoplast DNA maintenance and expression is associated with multi-drug resistance in Trypanosoma brucei in vitro [PDF]
It is well known that several antitrypanosomatid drugs accumulate in the parasite's mitochondrion, where they often bind to the organellar DNA, the kinetoplast.
A. Schnaufer +32 more
core +1 more source
A requirement for STAG2 in replication fork progression creates a targetable synthetic lethality in cohesin-mutant cancers. [PDF]
Cohesin is a multiprotein ring that is responsible for cohesion of sister chromatids and formation of DNA loops to regulate gene expression. Genomic analyses have identified that the cohesin subunit STAG2 is frequently inactivated by mutations in cancer.
Ashworth, Alan +4 more
core +2 more sources
Inhibition of Topoisomerase (DNA) I (TOP1): DNA Damage Repair and Anticancer Therapy
Most chemotherapy regimens contain at least one DNA-damaging agent that preferentially affects the growth of cancer cells. This strategy takes advantage of the differences in cell proliferation between normal and cancer cells.
Yang Xu, Chengtao Her
doaj +1 more source
Cancer is a disease that occurs as a result of abnormal or uncontrolled growth of cells due to DNA damage, among many other causes. Certain cancer treatments aim to increase the excess of DNA breaks to such an extent that they cannot escape from the ...
Ege Gok +6 more
doaj +1 more source
Topoisomerase expression and amplification in solid tumours: Analysis of 24,262 patients. [PDF]
BackgroundTopoisomerase I (TOPO1) and topoisomerase IIα (TOP2A) are specific targets of multiple chemotherapy drugs. Increased expression of TOPO1 protein and amplification of the TOP2A gene have been associated with treatment response in colorectal and ...
Arguello, David +4 more
core +1 more source
Long-term exposure to irinotecan reduces cell migration in glioma cells. [PDF]
In spite of considerable research into the therapies for glioblastoma multiforme this tumour type remains very difficult to treat. As well as having a tendency to be inherently resistant to chemotherapy, glioblastoma multiforme also displays local ...
Al-Ghafari, Ayat B. +6 more
core +1 more source
The DNA topoisomerase complement of Streptococcus pneumoniae is constituted by two type II enzymes (topoisomerase IV and gyrase), and a single type I enzyme (topoisomerase I).
Myriam V Valenzuela +5 more
doaj +1 more source

