Results 51 to 60 of about 32,790 (255)

Bulge oligonucleotide as an inhibitory agent of bacterial topoisomerase I

Journal of Enzyme Inhibition and Medicinal Chemistry, 2018
Bacterial topoisomerase I (Btopo I) was defined as potential target for discovery of new antibacterial compounds. Various oligonucleotides containing bulge structure were designed and synthesised as inhibitors to Btopo I in this investigation.
Zhaoqi Yang, Tuoyu Jiang, Hanshi Zhong, Yu Kang   +3 more
doaj   +1 more source

Crystal Structures of the 43 kDa ATPase Domain of Xanthomonas Oryzae pv. Oryzae Topoisomerase IV ParE Subunit and its Complex with Novobiocin

Crystals, 2019
Topoisomerase IV, one of the best-established antibacterial targets, is an enzyme crucial for chromosome segregation and cell division by catalyzing changes in DNA topology through breaking and rejoining DNA.
Ha Yun Jung, Yong-Seok Heo
doaj   +1 more source

Prostaglandins Isolated from the Octocoral Plexaura homomalla: In Silico and In Vitro Studies Against Different Enzymes of Cancer

Marine Drugs, 2020
Prostaglandin A2-AcMe (1) and Prostaglandin A2 (2) were isolated from the octocoral Plexaura homomalla and three semisynthetic derivatives (3−5) were then obtained using a reduction protocol.
Diana Ximena Hurtado, Fabio A. Castellanos, Ericsson Coy-Barrera, Edisson Tello   +3 more
doaj   +1 more source

Narciclasine, a novel topoisomerase I inhibitor, exhibited potent anti-cancer activity against cancer cells

Natural Products and Bioprospecting, 2023
DNA topoisomerases are essential nuclear enzymes in correcting topological DNA errors and maintaining DNA integrity. Topoisomerase inhibitors are a significant class of cancer chemotherapeutics with a definite curative effect. Natural products are a rich
Meichen Wang, Leilei Liang, Rong Wang, Shutao Jia, Chang Xu, Yuting Wang, Min Luo, Qiqi Lin, Min Yang, Hongyu Zhou, Dandan Liu, Chen Qing   +11 more
doaj   +1 more source

Topoisomerase I inhibitors: Review and update

Annals of Oncology, 1997
This review presents a summary of preclinical and clinical data on the topoisomerase I (topo I) inhibitors that are under clinical development. To date, all of the topo I inhibitors that have been clinically evaluated are analogues of camptothecin, an extract of the Chinese tree Camptotheca acuminata.
openaire   +2 more sources

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

Synthetic Approach to Hypoxyxylerone, Novel Inhibitor of Topoisomerase I. [PDF]

ChemInform, 2002
[reaction: see text] A potential route to the topoisomerase I inhibitor hypoxyxylerone is demonstrated by a highly convergent synthesis of the penta(O-methyl) derivative. The key step in the approach is an anionic homo-Fries rearrangement, little used to date in natural product synthesis and employed here for the first time with a dinaphthalenic ...
Arnaud, Piettre, Emmanuel, Chevenier, Christine, Massardier, Yves, Gimbert, Andrew E, Greene   +4 more
openaire   +2 more sources

Structure based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1 [PDF]

, 2014
The treatment of Human African Trypanosomiasis remains a major unmet health need in sub-Saharan Africa. Approaches involving new molecular targets are important and pteridine reductase 1 (PTR1), an enzyme that reduces dihydrobiopterin in Trypanosoma spp.
Kirsten Stewart, Michael P. Barrett, Pui Ee Wong, William N. Hunter, Barrack, Keri L., Hunter, William N., Huggan, Judith, Colin L. Gibson, Judith K. Huggan, Barrett, Michael P., Federica Giordani, Suckling, Colin J., Colin J. Suckling, Khalaf, Abedawn I., Huggan, Judith K., Wong, Pui Ee, Khalaf, Abedawn I, Barrack, Keri L, Stewart, Kirsten, Keri L. Barrack, Suckling, Colin J, Hunter, Wililam N., Gibson, Colin L., Giordani, Federica, Gibson, Colin L, Abedawn I. Khalaf, Hunter, William N   +26 more
core   +1 more source

Mitochondria and Neuromast Tagging With Fluorescent Gallium‐Triapine Analogues: In Cellulo MP FLIM and Zebrafish Live Imaging

Advanced Science, EarlyView.
Fluorescent BODIPY‐conjugated thiosemicarbazone ligands and their Ga(III), In(III), and Fe(III) complexes, inspired by Triapine, are developed as theranostic agents. Multiphoton FLIM and confocal microscopy in cancer cells and zebrafish reveal real‐time uptake, mitochondrial localisation, and whilst spectroscopic assays indicated preserved complex ...
Megan J. Green, Michael W. Jones, Merissa Saleem, Haobo Ge, Melita Tvardauskaite, Julia Dudzic, Fernando Cortezon‐Tamarit, Rory L. Arrowsmith, Charareh Pourzand, Gabriele Kociock‐Kohn, Nicholas H. Rees, Jonathan R. Dilworth, Stephen Faulkner, Stanley W. Botchway, David Gurevich, Sofia I. Pascu   +15 more
wiley   +1 more source

Tumor-targeted top1 inhibitor delivery with optimized parp inhibition in advanced solid tumors: a phase i trial of gapped scheduling

Nature Communications
Despite mechanistic rationale for combining PARP inhibitors with topoisomerase I inhibitors, clinical use has been hindered by dose-limiting toxicities.
Anish Thomas, Nobuyuki Takahashi, Lenka Oplustil O’Connor, Christophe E. Redon, Chirayu Mohindroo, Linda Sciuto, Lorinc Pongor, Keith T. Schmidt, Seth M. Steinberg, Mirit I. Aladjem, William Douglas Figg, Mark J. O’Connor, Yves Pommier   +12 more
doaj   +1 more source