dc.contributor.author | Constantinou, Andreas I. | en |
dc.contributor.author | Husband, A. | en |
dc.creator | Constantinou, Andreas I. | en |
dc.creator | Husband, A. | en |
dc.date.accessioned | 2019-11-04T12:50:22Z | |
dc.date.available | 2019-11-04T12:50:22Z | |
dc.date.issued | 2002 | |
dc.identifier.uri | http://gnosis.library.ucy.ac.cy/handle/7/52992 | |
dc.description.abstract | Cancer therapeutic drugs that inhibit DNA topoisomerase (topo) II by stabilizing the cleavable complex are collectively known as topo II poisons. Phenoxodiol is a synthetic derivative of the plant isoflavone daidzein and is currently undergoing clinical testing as a cancer therapeutic drug. The development of this agent as an antitumor drug was based to a large extent on its low toxicity in normal tissues but potent topo II inhibitory effects in rapidly dividing tumor cells. To evaluate phenoxodiol as a potential inhibitor of topoisomerases, we used the relaxation and nicking assays that can identify topo I inhibitors, and the unknotting and DNA cleavage assays that can identify topo II inhibitors. Phenoxodiol inhibited the catalytic activity of topo II in a dose-dependent manner and it stabilized the topo II-mediated cleavable complex, demonstrating that this agent is a topo II poison. Phenoxodiol's topo II inhibitory effects were comparable to those of other antitumor agents such as VP-16 and were stronger than those of genistein. Phenoxodiol did not inhibit topo I catalytic activity nor did it stabilize the topo I-mediated cleavable complex. These results demonstrate that phenoxodiol is a topo II-specific poison and suggest that this novel agent may find applications in cancer chemotherapy. | en |
dc.source | Anticancer Research | en |
dc.source.uri | https://www.scopus.com/inward/record.uri?eid=2-s2.0-0036765911&partnerID=40&md5=dcd2d3eb5c2ca9be3eb57a233e3adb93 | |
dc.subject | article | en |
dc.subject | antineoplastic agent | en |
dc.subject | Antineoplastic Agents | en |
dc.subject | etoposide | en |
dc.subject | human | en |
dc.subject | Humans | en |
dc.subject | controlled study | en |
dc.subject | priority journal | en |
dc.subject | dose response | en |
dc.subject | unclassified drug | en |
dc.subject | nonhuman | en |
dc.subject | DNA | en |
dc.subject | Enzyme Inhibitors | en |
dc.subject | DNA topoisomerase (ATP hydrolysing) | en |
dc.subject | enzyme inhibition | en |
dc.subject | molecular stability | en |
dc.subject | cancer inhibition | en |
dc.subject | catalysis | en |
dc.subject | Phenols | en |
dc.subject | DNA cleavage | en |
dc.subject | DNA Topoisomerases, Type II | en |
dc.subject | daidzein | en |
dc.subject | cell division | en |
dc.subject | DNA strand breakage | en |
dc.subject | Dose-Response Relationship, Drug | en |
dc.subject | isoflavone derivative | en |
dc.subject | Isoflavones | en |
dc.subject | cytotoxicity | en |
dc.subject | Antitumor drug | en |
dc.subject | Benzopyrans | en |
dc.subject | Cleavable complex | en |
dc.subject | DNA Damage | en |
dc.subject | DNA protein complex | en |
dc.subject | DNA supercoiling | en |
dc.subject | DNA topoisomerases | en |
dc.subject | DNA, Single-Stranded | en |
dc.subject | Isoflavone | en |
dc.subject | Nicking | en |
dc.subject | Phenoxodiol | en |
dc.subject | Relaxation | en |
dc.subject | Unknotting | en |
dc.title | Phenoxodiol (2H-1-benzopyran-7-0,1,3-(4-hydroxyphenyl)), a novel isoflavone derivative, inhibits DNA topoisomerase II by stabilizing the cleavable complex | en |
dc.type | info:eu-repo/semantics/article | |
dc.description.volume | 22 | |
dc.description.startingpage | 2581 | |
dc.description.endingpage | 2586 | |
dc.author.faculty | Σχολή Θετικών και Εφαρμοσμένων Επιστημών / Faculty of Pure and Applied Sciences | |
dc.author.department | Τμήμα Βιολογικών Επιστημών / Department of Biological Sciences | |
dc.type.uhtype | Article | en |
dc.description.notes | <p>Tradenames: vp 16, Sigma, United States | en |
dc.description.notes | Manufacturers: Indofine, United States | en |
dc.description.notes | Novogen, Australia | en |
dc.description.notes | Sigma, United States | en |
dc.description.notes | Cited By :44</p> | en |
dc.source.abbreviation | Anticancer Res. | en |
dc.contributor.orcid | Constantinou, Andreas I. [0000-0003-0365-1821] | |
dc.gnosis.orcid | 0000-0003-0365-1821 | |