Results 31 to 40 of about 29,245 (221)

PROSPECTS FOR SEARCHING MULTITARGET TOPOISOMERASE INHIBITORS WITH ANTITUMOR PROPERTIES

Сибирский онкологический журнал, 2019
Purpose of research: to identify the prospects of search for new antitumor non-camptothecin inhibitors of topoisomerase I/II among the various chemical compounds based on the analysis of side effects.Material and Methods.
M. I. Treshchalin, E. V. Neborak, H. M. Treshalina   +2 more
doaj   +1 more source

In Vitro Activity of Novel Topoisomerase Inhibitors against Francisella tularensis and Burkholderia pseudomallei

Antibiotics, 2023
Antimicrobial resistance is a global issue, and the investigation of alternative therapies that are not traditional antibiotics are warranted. Novel bacterial type II topoisomerase inhibitors (NBTIs) have recently emerged as a novel class of antibiotics ...
Adam O. Whelan, Ian Cooper, Nicola Ooi, David Orr, Kevin Blades, James Kirkham, Amanda Lyons, Kay B. Barnes, Mark I. Richards, Anne-Marie Salisbury, Mark Craighead, Sarah V. Harding   +11 more
doaj   +1 more source

Identification of a novel topoisomerase inhibitor effective in cells overexpressing drug efflux transporters. [PDF]

PLoS ONE, 2009
BACKGROUND:Natural product structures have high chemical diversity and are attractive as lead structures for discovery of new drugs. One of the disease areas where natural products are most frequently used as therapeutics is oncology. METHOD AND FINDINGS:
Walid Fayad, Mårten Fryknäs, Slavica Brnjic, Maria Hägg Olofsson, Rolf Larsson, Stig Linder   +5 more
doaj   +1 more source

The combined effects of proteasome inhibitor bortezomib with topoisomerase I and II inhibitors on topoisomerase enzymes

TURKISH JOURNAL OF MEDICAL SCIENCES, 2016
DNA topoisomerases are ubiquitous enzymes that regulate conformational changes in DNA topology during essential cellular processes, and, for this reason, have been characterized as the cellular targets of a number of anticancer drugs. Bortezomib is a powerful proteasome inhibitor used in the treatment of hematological malignancies.
Öksüzoğlu, Emine, Tırınoğlu, Çiydem, Kerimoğlu, Barış   +2 more
openaire   +3 more sources

Azacyanines as Novel Topoisomerase II Alpha Inhibitors

Letters in Drug Design & Discovery, 2020
Introduction:Topoisomerase II alpha (Topo IIα) has become one of the extensively exploited targets in chemotherapy due to its role in regulating the topological constraints of DNA during replication and transcription. Small molecules targeting Topo IIα’s activity such as etoposide (VP-16) and doxorubicin are extensively used in the treatment of many ...
Sercan Guloglu, Fahriye Nur Kirmaci, Özgül Persil Çetinkol, Mehrdad Forough, Aybuke Gulkaya   +4 more
openaire   +2 more sources

Discovery of New DNA Topoisomerase II Inhibitors using Structure Based Virtual Screening Method

Journal of the Turkish Chemical Society, Section A: Chemistry, 2019
DNA topoisomerases are proved therapeutic targets of anticancer and antibacterial drugs. Structures of topoisomerase–DNA and inhibitor ternary complexes have revealed the exact binding sites and mechanisms of topoisomerase poisons. There are two isoforms
Tugba Ertan-Bolelli, Kayhan Bolelli
doaj   +1 more source

Synthetic Inhibitors of DNA Topoisomerase I and II.

Chemical and Pharmaceutical Bulletin, 1999
A new type of synthetic inhibitor of DNA topoisomerase I and II was examined and several of these derivatives exhibited strong dual activity against these enzymes. This series of compounds showed high cytotoxic activities against cancer cells, but only a limited number of compounds showed any noticeable activity in an in vivo test against murine P388 ...
KATAYAMA, Hajime, KAWADA, Yusuke, KANEKO, Kimiyoshi, OSHIYAMA, Takamitsu, TAKATSU, Noriyuki   +4 more
openaire   +3 more sources

DNA-Binding Anticancer Drugs: One Target, Two Actions

Molecules, 2021
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, Catherine J. Drummond, Ying Yi Chen, Graeme J. Finlay   +3 more
doaj   +1 more source

MITF maintains genome stability in nonmelanocyte lineages

Molecular Oncology, EarlyView.
MITF is essential for melanocyte survival and acts as an oncogene in 10%–20% of melanomas. We show that MITF depletion causes genome instability in nonmelanocytic cells, leading to LATS2‐mediated P53 activation, cell cycle arrest, and apoptosis. This study highlights the role of MITF as a genome maintenance factor beyond the melanocyte lineage. Created
Drifa H. Gudmundsdottir, Adrián López García de Lomana, Thejus B. Venkatesh, Kritika Kirty, Snaevar Sigurdsson, Linda Vidarsdottir, Ramile Dilshat, Erla Sveinbjornsdottir, Snaedis Ragnarsdottir, Daniel H Magnusson, Maria R. Bustos, Eirikur Steingrimsson, Thorkell Gudjonsson, Stefan Sigurdsson   +13 more
wiley   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

FEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová, Grigorii Rakhalskii, Miroslav Almáši   +2 more
wiley   +1 more source