Results 41 to 50 of about 4,050,496 (258)

Novel DNA topoisomerase IIα inhibitors from combined ligand- and structure-based virtual screening.

PLoS ONE, 2014
DNA topoisomerases are enzymes responsible for the relaxation of DNA torsional strain, as well as for the untangling of DNA duplexes after replication, and are important cancer drug targets.
Malgorzata N Drwal, Jessica Marinello, Stefano G Manzo, Laurence P G Wakelin, Giovanni Capranico, Renate Griffith   +5 more
doaj   +1 more source

Clerocidin interacts with the cleavage complex of Streptococcus pneumoniae topoisomerase IV to induce selective irreversible DNA damage [PDF]

, 2006
Clerocidin (CL), a diterpenoid natural product, alkylates DNA through its epoxide moiety and exhibits both anticancer and antibacterial activities. We have examined CLaction in the presence of topoisomerase IV from Streptococcus pneumoniae.
Fisher, LM, RICHTER, SARA, Giaretta, G, LEO, ELISABETTA, GIARETTA, GIULIA, Palumbo, M, Leo, E, FISHER L. M, Richter, SN, Gatto, B, GATTO, BARBARA, PALUMBO, MANLIO   +11 more
core   +1 more source

Novel bacterial topoisomerase inhibitors derived from isomannide.

European journal of medicinal chemistry, 2020
A series of Novel Bacterial Topoisomerase Inhibitors (NBTIs) employing a linker derived from isomannide were synthesized and evaluated. Reduced hERG inhibition was observed compared to structure-matched analogues with different linkers, and compound 6 ...
A. Okumu, Yanran Lu, Sheri Dellos-Nolan, Jonathan L. Papa, Bryan J. Koci, Nicholas T. Cockroft, J. Gallucci, D. Wozniak, J. Yalowich, M. Mitton-Fry   +9 more
semanticscholar   +1 more source

Topoisomerase IIα promotes activation of RNA polymerase I transcription by facilitating pre-initiation complex formation [PDF]

, 2013
Type II DNA topoisomerases catalyse DNA double-strand cleavage, passage and re-ligation to effect topological changes. There is considerable interest in elucidating topoisomerase II roles, particularly as these proteins are targets for anti-cancer drugs.
Porter, Andrew C. G., Panov, Konstantin I; id_orcid, Zomerdijk, Joost C.B.M., Russell, J., Miller, G. (Gail), Zomerdijk, Joost C B M, Porter, A.C., Porter, Andrew C G, Volkov, A., Panov, K.I., Panov, Konstantin I., Russell, J. (Jackie), Panova, T., Zomerdijk, J.C., Miller, Gail, Porter, Andrew C.G., Miller, G., Panova, Tatiana, Russell, Jackie, Ray, S., Ray, Swagat, Volkov, Arsen, Zomerdijk, Joost C. B. M.   +22 more
core   +1 more source

On the viability of Escherichia coli cells lacking DNA topoisomerase I [PDF]

, 2012
Copyright @ 2012 Stockum et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution,
Lloyd, RG, Lloyd Robert G, Rudolph Christian J, Stockum Anna, Christian J Rudolph, Stockum, A, Anna Stockum, Robert G Lloyd, Rudolph, CJ   +8 more
core   +1 more source

Poly(ADP-Ribose) Polymerase (PARP) signaling of DNA damage induced by Topoisomerase 1 (TOP1) inhibition in carcinoma cells: chemotherapeutic implications of PARP and TOP1 inhibitors. [PDF]

, 2010
Una nuova strategia molecolare che incrementa l’azione antitumorale degli inibitori della Topoisomerasi 1 (TOP1) si basa sull’utilizzo di inibitori delle poli(ADP-ribosio) polimerasi (PARP).
D'Onofrio, Giovanna
core   +1 more source

Flavonoids and Their Derivatives as DNA Topoisomerase Inhibitors with Anti-Cancer Activity in Various Cell Models: Exploring a Novel Mode of Action.

Pharmacological Research
Flavonoids, a diverse group of plant-derived secondary metabolites, have garnered significant attention for their potential anti-cancer properties. This review explores the role of flavonoids as inhibitors of DNA topoisomerases, key enzymes essential for
P. Sitarek, Anna Merecz-Sadowska, Joanna Sikora, Malwina Dudzic, Natasza Wiertek-Płoszaj, Laurent Picot, T. Śliwiński, T. Kowalczyk   +7 more
semanticscholar   +1 more source

Inhibition of Poly(ADP-Ribose) polymerase enhances the toxicity of 131I-Metaiodobenzylguanidine/Topotecan combination therapy to cells and xenografts that express the noradrenaline transporter [PDF]

, 2012
Targeted radiotherapy using [131I]meta-iodobenzylguanidine ([131I]MIBG) has produced remissions in some neuroblastoma patients. We previously reported that combining [131I]MIBG with the topoisomerase I (Topo-I) inhibitor topotecan induced long-term DNA ...
McCluskey, Anthony G, Babich, John W, Champion, Sue, Mairs, Robert J, Boyd, Marie, Gaze, Mark N, Tesson, Mathias, Pimlott, Sally L   +7 more
core   +4 more sources

A Fine-Tuned Lipophilicity/Hydrophilicity Ratio Governs Antibacterial Potency and Selectivity of Bifurcated Halogen Bond-Forming NBTIs

Antibiotics, 2021
Herein, we report the design of a focused library of novel bacterial topoisomerase inhibitors (NBTIs) based on innovative mainly monocyclic right-hand side fragments active against DNA gyrase and Topo IV.
Anja Kolarič, Maja Kokot, Martina Hrast, Matjaž Weiss, Irena Zdovc, Jurij Trontelj, Simon Žakelj, Marko Anderluh, Nikola Minovski   +8 more
doaj   +1 more source

A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold

Molecules, 2018
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that mends topoisomerase 1-mediated DNA damage. Tdp1 is a current inhibition target for the development of improved anticancer treatments, as its inhibition may enhance the therapeutic effect ...
Nikolai S. Li-Zhulanov, Alexandra L. Zakharenko, Arina A. Chepanova, Jinal Patel, Ayesha Zafar, Konstantin P. Volcho, Nariman F. Salakhutdinov, Jóhannes Reynisson, Ivanhoe K. H. Leung, Olga I. Lavrik   +9 more
doaj   +1 more source