Targeting DNA Topoisomerase II in Antifungal Chemotherapy
Topoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Rais...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-11-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/22/7768 |
| _version_ | 1797464419913957376 |
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| author | Kavya Kondaka Iwona Gabriel |
| author_facet | Kavya Kondaka Iwona Gabriel |
| author_sort | Kavya Kondaka |
| collection | DOAJ |
| description | Topoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand the range of therapeutic options. In this review paper, we discussed the usefulness of fungal topo II as a molecular target for new drug discovery. On the basis of previously published data, we described structural and biochemical differences between fungal and human enzymes as well as a molecular basis of differential sensitivity to known anticancer drugs targeting the latter. This review focuses especially on highlighting the differences that may underlie the selectivity of action of new inhibitors. Distinct sites within fungal topo II in comparison with human counterparts are observed and should be further studied to understand the significance of those sites and their possible usage in design of new drugs. |
| first_indexed | 2024-03-09T18:07:54Z |
| format | Article |
| id | doaj.art-6006a4bdad1e4043b1a8aac5af2198a5 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T18:07:54Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-6006a4bdad1e4043b1a8aac5af2198a52023-11-24T09:20:48ZengMDPI AGMolecules1420-30492022-11-012722776810.3390/molecules27227768Targeting DNA Topoisomerase II in Antifungal ChemotherapyKavya Kondaka0Iwona Gabriel1Department of Pharmaceutical Technology and Biochemistry, Gdansk University of Technology, 80-233 Gdansk, PolandDepartment of Pharmaceutical Technology and Biochemistry, Gdansk University of Technology, 80-233 Gdansk, PolandTopoisomerase inhibitors have been in use clinically for the treatment of several diseases for decades. Although those enzymes are significant molecular targets in antibacterial and anticancer chemotherapy very little is known about the possibilities to target fungal topoisomerase II (topo II). Raising concern for the fungal infections, lack of effective drugs and a phenomenon of multidrug resistance underlie a strong need to expand the range of therapeutic options. In this review paper, we discussed the usefulness of fungal topo II as a molecular target for new drug discovery. On the basis of previously published data, we described structural and biochemical differences between fungal and human enzymes as well as a molecular basis of differential sensitivity to known anticancer drugs targeting the latter. This review focuses especially on highlighting the differences that may underlie the selectivity of action of new inhibitors. Distinct sites within fungal topo II in comparison with human counterparts are observed and should be further studied to understand the significance of those sites and their possible usage in design of new drugs.https://www.mdpi.com/1420-3049/27/22/7768antifungalsyeast topoisomerase 2inhibitordifferential sensitivitypotential drugs |
| spellingShingle | Kavya Kondaka Iwona Gabriel Targeting DNA Topoisomerase II in Antifungal Chemotherapy Molecules antifungals yeast topoisomerase 2 inhibitor differential sensitivity potential drugs |
| title | Targeting DNA Topoisomerase II in Antifungal Chemotherapy |
| title_full | Targeting DNA Topoisomerase II in Antifungal Chemotherapy |
| title_fullStr | Targeting DNA Topoisomerase II in Antifungal Chemotherapy |
| title_full_unstemmed | Targeting DNA Topoisomerase II in Antifungal Chemotherapy |
| title_short | Targeting DNA Topoisomerase II in Antifungal Chemotherapy |
| title_sort | targeting dna topoisomerase ii in antifungal chemotherapy |
| topic | antifungals yeast topoisomerase 2 inhibitor differential sensitivity potential drugs |
| url | https://www.mdpi.com/1420-3049/27/22/7768 |
| work_keys_str_mv | AT kavyakondaka targetingdnatopoisomeraseiiinantifungalchemotherapy AT iwonagabriel targetingdnatopoisomeraseiiinantifungalchemotherapy |