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Combination of PARPi and topoisomerase I inhibitors is highly effective in olaparib-resistant ovarian cancer. [PDF]

Exp Hematol Oncol
Chiappa M, Villa V, Sias F, Grasselli C, Sala L, Canesi S, Marabese M, Mason S, Dibitetto D, Fruscio R, Damia G.   +10 more
europepmc   +1 more source

Recent Advances in Use of Topoisomerase Inhibitors in Combination Cancer Therapy.

Current Topics in Medicinal Chemistry, 2019
Inhibitors targeting human topoisomerase I and topoisomerase II alpha have provided a useful chemotherapy option for treatment of many patients suffering from a variety of cancers.
Wen-Jie Wang, Y. Tse-Dinh
semanticscholar   +2 more sources

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Topoisomerase II inhibitors design: Early studies and new perspectives.

Bioorganic chemistry (Print), 2023
The DNA topoisomerase enzymes are widely distributed throughout all spheres of life and are necessary for cell function. Numerous antibacterial and cancer chemotherapeutic drugs target the various topoisomerase enzymes because of their roles in ...
Hadeer K. Swedan, Asmaa E. Kassab, E. M. Gedawy, S. Elmeligie   +3 more
semanticscholar   +1 more source

The design and discovery of topoisomerase I inhibitors as anticancer therapies

Expert Opinion on Drug Discovery, 2022
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 the relaxation of supercoiled DNA.
Endika Martin-Encinas, Asier Selas, Francisco Palacios, C. Alonso   +3 more
semanticscholar   +1 more source

Design, synthesis, and antibacterial evaluation of new quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids as potential inhibitors of DNA gyrase and topoisomerase IV.

Bioorganic chemistry (Print), 2021
DNA gyrase and topoisomerase IV (topo IV) inhibitors are among the most interesting antibacterial drug classes without antibacterial pipeline representative.
Heba A. Hofny, M. Mohamed, H. Gomaa, Salah Abdel-aziz, B. Youssif, N. El-Koussi, Ahmed S. Aboraia   +6 more
semanticscholar   +1 more source

Recent advancements in the medicinal chemistry of bacterial type II topoisomerase inhibitors.

Bioorganic chemistry (Print), 2020
Replication proteins are sought as a potential targets for antimicrobial agents. Despite their promising target characteristics, only topoisomerase II inhibitors targeting DNA gyrase and/or topoisomerase IV have reached clinical use.
S. Jaswal, Bhupender Nehra, Shubham Kumar, Vikramdeep Monga   +3 more
semanticscholar   +1 more source

A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade.

European journal of medicinal chemistry, 2019
The topoisomerase enzymes play an important role in DNA metabolism, and searching for enzyme inhibitors is an important target in the search for new anticancer drugs.
Xiao-Xia Liang, Qiang Wu, Shangxian Luan, Z. Yin, Chang-liang He, Li-Zi Yin, Yuan-Feng Zou, Zhi-Xiang Yuan, Li-Xia Li, Xu Song, Min He, Cheng Lv, Wei Zhang   +12 more
semanticscholar   +1 more source

A patent review of topoisomerase I inhibitors (2016–present)

Expert Opinion on Therapeutic Patents, 2021
Introduction Topoisomerases are important targets for therapeutic improvement in the treatment of some diseases, including cancer. Inhibitors and poisons of topoisomerase I can limit the activity of this enzyme in its enzymatic cycle.
Asier Selas, Endika Martin-Encinas, Maria Fuertes, C. Masdeu, G. Rubiales, F. Palacios, C. Alonso   +6 more
semanticscholar   +1 more source

Recent progress in topoisomerase inhibitors as anticancer agents: Research and design strategies for Topo I and II inhibitors via structural optimization.

Bioorganic chemistry (Print)
Topoisomerase (Topo) is a crucial class of enzymes that play significant roles in DNA replication, transcription, and repair. Epidemiological research has highlighted the necessity of topoisomerase for the proliferation and genomic stability of tumor ...
Guang-Huan Shen, Shihao Li, Yu Zhu, Zheng Xu, Xuan Liu, Chun-Yan Lv, Zhi-Hua Xing, Lin-Lin Cui, Wenlan Li   +8 more
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