Results 11 to 20 of about 146,499 (323)
DNA-Binding Anticancer Drugs: One Target, Two Actions
Amsacrine, an anticancer drug first synthesised in 1970 by Professor Cain and colleagues, showed excellent preclinical activity and underwent clinical trial in 1978 under the auspices of the US National Cancer Institute, showing activity against acute ...
Bruce C. Baguley +3 more
doaj +1 more source
Bacterial Topoisomerases, Anti‐Topoisomerases, and Anti‐Topoisomerase Resistance [PDF]
Topoisomerases are ubiquitous enzymes necessary for controlling the interlinking and twisting of DNA molecules. Among the four topoisomerases identified in eubacteria, two, DNA gyrase and topoisomerase IV have been exploited by nature and the pharmaceutical industry as antibacterial targets.
openaire +2 more sources
Synthesis and Biological Evaluation of Novel Indole-Derived Thioureas
A series of 2-(1H-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1H-indol-3-yl)ethanamine with appropriate aryl/alkylisothiocyanates in anhydrous media.
Giuseppina Sanna +13 more
doaj +1 more source
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 +1 more source
Fluoroquinolones are synthetic antibacterial agents that stabilize the ternary complex of prokaryotic topoisomerase II enzymes (gyrase and Topo IV), leading to extensive DNA fragmentation and bacteria death.
Temilolu Idowu, Frank Schweizer
doaj +1 more source
Distinct requirements for the Rad32(Mre¹¹) nuclease and Ctp1(CtIP) in the removal of covalently bound topoisomerase I and II from DNA [PDF]
For a cancer cell to resist treatment with drugs that trap topoisomerases covalently on the DNA, the topoisomerase must be removed. In this study, we provide evidence that the Schizosaccharomyces pombe Rad32Mre11 nuclease activity is involved in the ...
Akamatsu +38 more
core +2 more sources
A nucleotide resolution map of Top2-linked DNA breaks in the yeast and human genome [PDF]
DNA topoisomerases are required to resolve DNA topological stress. Despite this essential role, abortive topoisomerase activity generates aberrant protein-linked DNA breaks, jeopardising genome stability.
Allison, Rachal M +5 more
core +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
TDP1/TOP1 ratio as a promising indicator for the response of small cell lung cancer to topotecan [PDF]
BACKGROUND AND OBJECTIVE Small cell lung cancer (SCLC) is one of the most challenging tumors to treat due to high proliferation rate, early metastatic dissemination and rapid development of chemotherapy resistance.
El-Khamisy, Sherif F +3 more
core +3 more sources
A comparative study of topoisomerase activity in two European crayfish species Astacus astacus and Austropotamobius pallipes was carried out to determine the physiological basis of the difference in ecological fitness of these systematically related ...
PAOLUCCI M. +3 more
doaj +1 more source

