Results 21 to 30 of about 4,050,496 (258)

Novel Bacterial Topoisomerase inhibitors (NBTIs) – A comprehensive review

European Journal of Medicinal Chemistry Reports, 2021
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria.
Jigar Desai, Sachchidanand S, Sanjay Kumar, Rajiv Sharma   +3 more
doaj   +1 more source

The Potential of Topoisomerase Inhibitor-Based Antibody–Drug Conjugates

Pharmaceutics, 2022
DNA topoisomerases are essential enzymes that stabilize DNA supercoiling and resolve entanglements. Topoisomerase inhibitors have been widely used as anti-cancer drugs for the past 20 years.
Seungmin Han, Kwang Suk Lim, Brody J. Blackburn, Jina Yun, Charles W. Putnam, David A. Bull, Young-Wook Won   +6 more
doaj   +1 more source

Topoisomerase-II mediated biochemical mapping of centromeres and nitroreductase mediated drug metabolism in Trypanosomatids [PDF]

, 2012
PhDThe protozoan parasites Trypanosoma cruzi and Trypanosoma brucei are the causative agents of Chagas disease and Human African sleeping sickness respectively.
Bot, Christopher
core   +4 more sources

The chemotherapeutic CX-5461 primarily targets TOP2B and exhibits selective activity in high-risk neuroblastoma

Nature Communications, 2021
CX-5461 recently progressed through phase I clinical trial as a first-inhuman inhibitor of RNA-POL I. Here, the authors demonstrate that CX-5461 synergizes with topoisomerase I inhibitors to inhibit neuroblastoma cells and that its primary target in this
Min Pan, William C. Wright, Richard H. Chapple, Asif Zubair, Manbir Sandhu, Jake E. Batchelder, Brandt C. Huddle, Jonathan Low, Kaley B. Blankenship, Yingzhe Wang, Brittney Gordon, Payton Archer, Samuel W. Brady, Sivaraman Natarajan, Matthew J. Posgai, John Schuetz, Darcie Miller, Ravi Kalathur, Siquan Chen, Jon Patrick Connelly, M. Madan Babu, Michael A. Dyer, Shondra M. Pruett-Miller, Burgess B. Freeman, Taosheng Chen, Lucy A. Godley, Scott C. Blanchard, Elizabeth Stewart, John Easton, Paul Geeleher   +29 more
doaj   +1 more source

MRE11 facilitates the removal of human topoisomerase II complexes from genomic DNA [PDF]

, 2012
Topoisomerase II creates a double-strand break intermediate with topoisomerase covalently coupled to the DNA via a 5'-phosphotyrosyl bond. These intermediate complexes can become cytotoxic protein-DNA adducts and DSB repair at these lesions requires ...
Caroline A. Austin, Graham H. Jackson, Nicholas J. Morris, Zbyslaw Sondka, Tainer, JA, Padget, Kay, Simon J. Cockell, Curtis, H, Cockell, SJ, Curtis, Hannah, Sondka, Zbyslaw, Austin, CA, John A. Tainer, Cowell, IG, Austin, Caroline, Padget, K, Morris, Nicholas, Moiani, Davide, Cowell, Ian, Ian G. Cowell, Sondka, Z, Lee, KC, Tainer, John, Jackson, Graham, Kay Padget, Moiani, D, Lee, Ka Cheong, Jackson, GH, Ka Cheong Lee, Davide Moiani, Hannah Curtis, Morris, NJ, Cockell, Simon   +32 more
core   +1 more source

15-deoxy-Δ12, 14-prostaglandin J2 enhances anticancer activities independently of VHL status in renal cell carcinomas

Biochemistry and Biophysics Reports, 2019
Renal cell carcinoma (RCC) is relatively resistant to chemotherapy and radiotherapy. Clear cell RCC (ccRCC) accounts for the majority of RCC, which have mutations or epigenetic silencing of the von Hippel–Lindau (VHL) gene.
Hiromi Koma, Yasuhiro Yamamoto, Tomonari Fujita, Tatsurou Yagami   +3 more
doaj   +1 more source

The impact of the C-terminal domain on the interaction of human DNA topoisomerase II α and β with DNA [PDF]

, 2011
<b>Background</b> Type II DNA topoisomerases are essential, ubiquitous enzymes that act to relieve topological problems arising in DNA from normal cellular activity.
Caroline A. Austin, Kathryn L Gilroy, Caroline A Austin, Austin Caroline A., Austin, C.A., Gilroy Kathryn L., Gilroy, K.L., Kathryn L. Gilroy   +7 more
core   +2 more sources

Application of a novel microtitre plate-based assay for the discovery of new inhibitors of DNA gyrase and DNA topoisomerase VI.

PLoS ONE, 2013
DNA topoisomerases are highly exploited targets for antimicrobial drugs. The spread of antibiotic resistance represents a significant threat to public health and necessitates the discovery of inhibitors that target topoisomerases in novel ways.
James A Taylor, Lesley A Mitchenall, Martin Rejzek, Robert A Field, Anthony Maxwell   +4 more
doaj   +1 more source

Structural Basis of Gate-DNA Breakage and Resealing by Type II Topoisomerases [PDF]

, 2010
ype II DNA topoisomerases are ubiquitous enzymes with essential functions in DNA replication, recombination and transcription. They change DNA topology by forming a transient covalent cleavage complex with a gate-DNA duplex that allows transport of a ...
Laponogov, I, Fisher L. Mark, Pan, Xiao-Su, Sanderson, MR, Xiao-Su Pan, Katherine E McAuley, Fisher, LM, McAuley, Katherine E., McAuley, KE, Pan Xiao-Su, Veselkov, Dennis A., Ivan Laponogov, Mark R. Sanderson, Veselkov Dennis A., Sanderson Mark R., L Mark Fisher, Veselkov, DA, Mark R Sanderson, Fisher, L. Mark, Dennis A. Veselkov, Katherine E. McAuley, Laponogov Ivan, Sanderson, Mark R., Laponogov, Ivan, McAuley Katherine E., Dennis A Veselkov, Pan, XS, L. Mark Fisher   +27 more
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First-in-Class, Thiosemicarbazide-Based, Dual Inhibitors of Human DNA Topoisomerase IIα and Indoleamine-2,3-Dioxygenase 1 (IDO-1) with Strong Anticancer Properties

Medical Sciences Forum, 2022
According to a WHO report from 2020, cancer constitutes one of the leading causes of death worldwide. The number of cancer deaths is estimated to be approximately 10 million per year.
Barbara Kaproń, Tomasz Plech
doaj   +1 more source