Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity
Hsien-Ya Lin, Chia-Yu Chen, Ting-Chien Lin and colleagues perform structure-guided modifications of the compound uronic isofagomaine in order to engineer a highly specific and potent inhibitor of gut bacterial β-glucuronidases (GUSs). The authors present eight crystal structures and demonstrate in v...
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Nature Portfolio
2021
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oai:doaj.org-article:fb39bb5584a546bea3aca76fb3fd4c022021-12-02T13:19:27ZEntropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity10.1038/s42003-021-01815-w2399-3642https://doaj.org/article/fb39bb5584a546bea3aca76fb3fd4c022021-03-01T00:00:00Zhttps://doi.org/10.1038/s42003-021-01815-whttps://doaj.org/toc/2399-3642Hsien-Ya Lin, Chia-Yu Chen, Ting-Chien Lin and colleagues perform structure-guided modifications of the compound uronic isofagomaine in order to engineer a highly specific and potent inhibitor of gut bacterial β-glucuronidases (GUSs). The authors present eight crystal structures and demonstrate in vivo efficacy of the optimised C6-alkyl derivative inhibitor in mice models. This study may enhance the development of inhibitors of microbial GUS for use in colorectal cancer therapy to minimize the undesired side effects of irinotecan treatment.Hsien-Ya LinChia-Yu ChenTing-Chien LinLun-Fu YehWei-Che HsiehShijay GaoPierre-Alain BurnoufBing-Mae ChenTung-Ju HsiehPunsaldulam DashnyamYen-Hsi KuoZhijay TuSteve R. RofflerChun-Hung LinNature PortfolioarticleBiology (General)QH301-705.5ENCommunications Biology, Vol 4, Iss 1, Pp 1-10 (2021) |
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| topic |
Biology (General) QH301-705.5 |
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Biology (General) QH301-705.5 Hsien-Ya Lin Chia-Yu Chen Ting-Chien Lin Lun-Fu Yeh Wei-Che Hsieh Shijay Gao Pierre-Alain Burnouf Bing-Mae Chen Tung-Ju Hsieh Punsaldulam Dashnyam Yen-Hsi Kuo Zhijay Tu Steve R. Roffler Chun-Hung Lin Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| description |
Hsien-Ya Lin, Chia-Yu Chen, Ting-Chien Lin and colleagues perform structure-guided modifications of the compound uronic isofagomaine in order to engineer a highly specific and potent inhibitor of gut bacterial β-glucuronidases (GUSs). The authors present eight crystal structures and demonstrate in vivo efficacy of the optimised C6-alkyl derivative inhibitor in mice models. This study may enhance the development of inhibitors of microbial GUS for use in colorectal cancer therapy to minimize the undesired side effects of irinotecan treatment. |
| format |
article |
| author |
Hsien-Ya Lin Chia-Yu Chen Ting-Chien Lin Lun-Fu Yeh Wei-Che Hsieh Shijay Gao Pierre-Alain Burnouf Bing-Mae Chen Tung-Ju Hsieh Punsaldulam Dashnyam Yen-Hsi Kuo Zhijay Tu Steve R. Roffler Chun-Hung Lin |
| author_facet |
Hsien-Ya Lin Chia-Yu Chen Ting-Chien Lin Lun-Fu Yeh Wei-Che Hsieh Shijay Gao Pierre-Alain Burnouf Bing-Mae Chen Tung-Ju Hsieh Punsaldulam Dashnyam Yen-Hsi Kuo Zhijay Tu Steve R. Roffler Chun-Hung Lin |
| author_sort |
Hsien-Ya Lin |
| title |
Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| title_short |
Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| title_full |
Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| title_fullStr |
Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| title_full_unstemmed |
Entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| title_sort |
entropy-driven binding of gut bacterial β-glucuronidase inhibitors ameliorates irinotecan-induced toxicity |
| publisher |
Nature Portfolio |
| publishDate |
2021 |
| url |
https://doaj.org/article/fb39bb5584a546bea3aca76fb3fd4c02 |
| work_keys_str_mv |
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1718393308673212416 |