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From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica
Nature has been always a great source of possible lead compounds to develop new drugs against several diseases. Here we report the identification of a natural compound, membranoid G, derived from the Antarctic sponge Dendrilla antarctica displaying an in vitro inhibitory activity against human DNA t...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Taylor & Francis
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9132426/ https://www.ncbi.nlm.nih.gov/pubmed/35603503 http://dx.doi.org/10.1080/14756366.2022.2078320 |
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author | Ottaviani, Alessio Welsch, Joshua Agama, Keli Pommier, Yves Desideri, Alessandro Baker, Bill J. Fiorani, Paola |
author_facet | Ottaviani, Alessio Welsch, Joshua Agama, Keli Pommier, Yves Desideri, Alessandro Baker, Bill J. Fiorani, Paola |
author_sort | Ottaviani, Alessio |
collection | PubMed |
description | Nature has been always a great source of possible lead compounds to develop new drugs against several diseases. Here we report the identification of a natural compound, membranoid G, derived from the Antarctic sponge Dendrilla antarctica displaying an in vitro inhibitory activity against human DNA topoisomerase 1B. The experiments indicate that membranoid G, when pre-incubated with the enzyme, strongly and irreversibly inhibits the relaxation of supercoiled DNA. This compound completely inhibits the cleavage step of the enzyme catalytic mechanism by preventing protein binding to the DNA. Membranoid G displays also a cytotoxic effect on tumour cell lines, suggesting its use as a possible lead compound to develop new anticancer drugs. |
format | Online Article Text |
id | pubmed-9132426 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Taylor & Francis |
record_format | MEDLINE/PubMed |
spelling | pubmed-91324262022-05-26 From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica Ottaviani, Alessio Welsch, Joshua Agama, Keli Pommier, Yves Desideri, Alessandro Baker, Bill J. Fiorani, Paola J Enzyme Inhib Med Chem Brief Report Nature has been always a great source of possible lead compounds to develop new drugs against several diseases. Here we report the identification of a natural compound, membranoid G, derived from the Antarctic sponge Dendrilla antarctica displaying an in vitro inhibitory activity against human DNA topoisomerase 1B. The experiments indicate that membranoid G, when pre-incubated with the enzyme, strongly and irreversibly inhibits the relaxation of supercoiled DNA. This compound completely inhibits the cleavage step of the enzyme catalytic mechanism by preventing protein binding to the DNA. Membranoid G displays also a cytotoxic effect on tumour cell lines, suggesting its use as a possible lead compound to develop new anticancer drugs. Taylor & Francis 2022-05-23 /pmc/articles/PMC9132426/ /pubmed/35603503 http://dx.doi.org/10.1080/14756366.2022.2078320 Text en © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Brief Report Ottaviani, Alessio Welsch, Joshua Agama, Keli Pommier, Yves Desideri, Alessandro Baker, Bill J. Fiorani, Paola From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title | From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title_full | From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title_fullStr | From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title_full_unstemmed | From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title_short | From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
title_sort | from antarctica to cancer research: a novel human dna topoisomerase 1b inhibitor from antarctic sponge dendrilla antarctica |
topic | Brief Report |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9132426/ https://www.ncbi.nlm.nih.gov/pubmed/35603503 http://dx.doi.org/10.1080/14756366.2022.2078320 |
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