Topoisomerase I inhibitors: Challenges, progress and the road ahead

A Talukdar, B Kundu, D Sarkar, S Goon… - European Journal of …, 2022 - Elsevier
Abstract Topoisomerase IB (Top1), a subcategory of DNA topoisomerase enzymes is
expressed much higher in several tumor cells. Therefore, modulating the activity of Top1 in …

DNA topoisomerases as molecular targets for anticancer drugs

K Buzun, A Bielawska, K Bielawski… - Journal of Enzyme …, 2020 - Taylor & Francis
The significant role of topoisomerases in the control of DNA chain topology has been
confirmed in numerous research conducted worldwide. The prevalence of these enzymes …

Six‐Membered Aromatic Nitrogen Heterocyclic Anti‐Tumor Agents: Synthesis and Applications

J Li, A Gu, XM Nong, S Zhai, ZY Yue… - The Chemical …, 2023 - Wiley Online Library
Cancer stands as a serious malady, posing substantial risks to human well‐being and
survival. This underscores the paramount necessity to explore and investigate novel …

The design and discovery of topoisomerase I inhibitors as anticancer therapies

E Martín-Encinas, A Selas, F Palacios… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Cancer has been identified as one of the leading causes of death worldwide.
The biological target of some anticancer agents is topoisomerase I, an enzyme involved in …

Design, synthesis, and biological evaluation of 3, 3′-diindolylmethane N-linked glycoconjugate as a leishmanial topoisomerase IB inhibitor with reduced cytotoxicity

P Kour, P Saha, S Bhattacharya, D Kumari… - RSC Medicinal …, 2023 - pubs.rsc.org
Leishmaniasis, one of the neglected diseases, ranks second to malaria in the cause of
parasitic mortality and morbidity. The present chemotherapeutic regimen faces the …

Copper(I)-Catalyzed Nitrile-Addition/N-Arylation Ring-Closure Cascade: Synthesis of 5,11-Dihydro-6H-indolo[3,2-c]quinolin-6-ones as Potent Topoisomerase-I …

WY Hsueh, YSE Lee, MS Huang, CH Lai… - Journal of Medicinal …, 2021 - ACS Publications
In this paper, we present a copper (I)-catalyzed nitrile-addition/N-arylation ring-closure
cascade for the synthesis of 5, 11-dihydro-6 H-indolo [3, 2-c] quinolin-6-ones from 2-(2 …

[HTML][HTML] Natural compounds as therapeutic agents: The case of human topoisomerase ib

A Ottaviani, F Iacovelli, P Fiorani… - International Journal of …, 2021 - mdpi.com
Natural products are widely used as source for drugs development. An interesting example
is represented by natural drugs developed against human topoisomerase IB, a ubiquitous …

Emerging roles of DNA topoisomerases in the regulation of R-loops

PS Patel, R Krishnan, R Hakem - Mutation Research/Genetic Toxicology …, 2022 - Elsevier
R-loops are comprised of a DNA: RNA hybrid and a displaced single-strand DNA (ssDNA)
that reinvades the DNA duplex behind the moving RNA polymerase. Because they have …

G-quadruplex-containing oligodeoxynucleotides as DNA topoisomerase I inhibitors

D Li, X Chen, R Yan, Z Jiang, B Zhou, B Lv - International Journal of …, 2022 - Elsevier
DNA topoisomerase I was found to be highly abundant in fast-proliferating tumor cells and is
a potential target for anticancer therapy. A series of G-quadruplex-containing …

Topoisomerase assays

JL Nitiss, K Kiianitsa, Y Sun, KC Nitiss… - Current …, 2021 - Wiley Online Library
Topoisomerases are enzymes that play essential roles in DNA replication, transcription,
chromosome segregation, and recombination. All cells have two major forms of DNA …