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...
Published in: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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Taylor & Francis Group
2022
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Online Access: | https://doi.org/10.1080/14756366.2022.2078320 https://doaj.org/article/5842509fe50740f0bb3a4e4b31f70e4f |
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ftdoajarticles:oai:doaj.org/article:5842509fe50740f0bb3a4e4b31f70e4f 2023-05-15T13:51:32+02:00 From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica Alessio Ottaviani Joshua Welsch Keli Agama Yves Pommier Alessandro Desideri Bill J. Baker Paola Fiorani 2022-12-01T00:00:00Z https://doi.org/10.1080/14756366.2022.2078320 https://doaj.org/article/5842509fe50740f0bb3a4e4b31f70e4f EN eng Taylor & Francis Group https://www.tandfonline.com/doi/10.1080/14756366.2022.2078320 https://doaj.org/toc/1475-6366 https://doaj.org/toc/1475-6374 doi:10.1080/14756366.2022.2078320 1475-6374 1475-6366 https://doaj.org/article/5842509fe50740f0bb3a4e4b31f70e4f Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1404-1410 (2022) Natural product topoisomerase cancer drug development Therapeutics. Pharmacology RM1-950 article 2022 ftdoajarticles https://doi.org/10.1080/14756366.2022.2078320 2022-12-30T21:47:57Z 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. Article in Journal/Newspaper Antarc* Antarctic Antarctica Directory of Open Access Journals: DOAJ Articles Antarctic The Antarctic Journal of Enzyme Inhibition and Medicinal Chemistry 37 1 1404 1410 |
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Open Polar |
collection |
Directory of Open Access Journals: DOAJ Articles |
op_collection_id |
ftdoajarticles |
language |
English |
topic |
Natural product topoisomerase cancer drug development Therapeutics. Pharmacology RM1-950 |
spellingShingle |
Natural product topoisomerase cancer drug development Therapeutics. Pharmacology RM1-950 Alessio Ottaviani Joshua Welsch Keli Agama Yves Pommier Alessandro Desideri Bill J. Baker Paola Fiorani From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica |
topic_facet |
Natural product topoisomerase cancer drug development Therapeutics. Pharmacology RM1-950 |
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 |
Article in Journal/Newspaper |
author |
Alessio Ottaviani Joshua Welsch Keli Agama Yves Pommier Alessandro Desideri Bill J. Baker Paola Fiorani |
author_facet |
Alessio Ottaviani Joshua Welsch Keli Agama Yves Pommier Alessandro Desideri Bill J. Baker Paola Fiorani |
author_sort |
Alessio Ottaviani |
title |
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_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_sort |
from antarctica to cancer research: a novel human dna topoisomerase 1b inhibitor from antarctic sponge dendrilla antarctica |
publisher |
Taylor & Francis Group |
publishDate |
2022 |
url |
https://doi.org/10.1080/14756366.2022.2078320 https://doaj.org/article/5842509fe50740f0bb3a4e4b31f70e4f |
geographic |
Antarctic The Antarctic |
geographic_facet |
Antarctic The Antarctic |
genre |
Antarc* Antarctic Antarctica |
genre_facet |
Antarc* Antarctic Antarctica |
op_source |
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1404-1410 (2022) |
op_relation |
https://www.tandfonline.com/doi/10.1080/14756366.2022.2078320 https://doaj.org/toc/1475-6366 https://doaj.org/toc/1475-6374 doi:10.1080/14756366.2022.2078320 1475-6374 1475-6366 https://doaj.org/article/5842509fe50740f0bb3a4e4b31f70e4f |
op_doi |
https://doi.org/10.1080/14756366.2022.2078320 |
container_title |
Journal of Enzyme Inhibition and Medicinal Chemistry |
container_volume |
37 |
container_issue |
1 |
container_start_page |
1404 |
op_container_end_page |
1410 |
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1766255440742580224 |