Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides
The biosynthesis of polyene macrolides, which are natural products produced by soil actinomycetes, have been extensively explored, and recent studies have focused on the effects of post–polyketide synthase (PKS) modifications to polyene macrolides on toxicity, water solubility, and antifungal activi...
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MDPI AG
2023-01-01
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Series: | Antibiotics |
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Online Access: | https://www.mdpi.com/2079-6382/12/1/119 |
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author | Liqin Qiao Yao Dong Hongli Zhou Hao Cui |
author_facet | Liqin Qiao Yao Dong Hongli Zhou Hao Cui |
author_sort | Liqin Qiao |
collection | DOAJ |
description | The biosynthesis of polyene macrolides, which are natural products produced by soil actinomycetes, have been extensively explored, and recent studies have focused on the effects of post–polyketide synthase (PKS) modifications to polyene macrolides on toxicity, water solubility, and antifungal activity. For example, there are interactions between glycosyl, carboxyl, and hydroxyl or epoxy groups generated in the post-PKS modification steps; salt bridges will be formed between carboxylate and ammonium on the mycosamine; and water bridges will be formed between hydroxy and hydroxyl on mycosamine. These interactions will affect their water solubility and substrate-recognition specificity. This review summarizes research related to these post-PKS modification groups and discusses some genetic engineering operation problems and solutions that may be encountered when modifying these post-PKS modification groups. In addition, this review provides a basis for the structural research of polyene macrolide antibiotics and contributes to comprehensive and systematic knowledge, and it may thus encourage researchers to develop novel antifungal drugs with higher therapeutic indexes and medical values. |
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language | English |
last_indexed | 2024-03-09T13:47:56Z |
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series | Antibiotics |
spelling | doaj.art-2ef2c497e6bf4a578f82e9680a3738102023-11-30T20:56:00ZengMDPI AGAntibiotics2079-63822023-01-0112111910.3390/antibiotics12010119Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene MacrolidesLiqin Qiao0Yao Dong1Hongli Zhou2Hao Cui3School of Chemistry and Pharmaceutical Engineering, Jilin Institute of Chemical Technology, Jilin 132022, ChinaCollege of Biology & Food Engineering, Jilin Institute of Chemical Technology, Jilin 132022, ChinaSchool of Chemistry and Pharmaceutical Engineering, Jilin Institute of Chemical Technology, Jilin 132022, ChinaSchool of Chemistry and Pharmaceutical Engineering, Jilin Institute of Chemical Technology, Jilin 132022, ChinaThe biosynthesis of polyene macrolides, which are natural products produced by soil actinomycetes, have been extensively explored, and recent studies have focused on the effects of post–polyketide synthase (PKS) modifications to polyene macrolides on toxicity, water solubility, and antifungal activity. For example, there are interactions between glycosyl, carboxyl, and hydroxyl or epoxy groups generated in the post-PKS modification steps; salt bridges will be formed between carboxylate and ammonium on the mycosamine; and water bridges will be formed between hydroxy and hydroxyl on mycosamine. These interactions will affect their water solubility and substrate-recognition specificity. This review summarizes research related to these post-PKS modification groups and discusses some genetic engineering operation problems and solutions that may be encountered when modifying these post-PKS modification groups. In addition, this review provides a basis for the structural research of polyene macrolide antibiotics and contributes to comprehensive and systematic knowledge, and it may thus encourage researchers to develop novel antifungal drugs with higher therapeutic indexes and medical values.https://www.mdpi.com/2079-6382/12/1/119polyene macrolidespost-PKS modificationspropertyantifungal activity |
spellingShingle | Liqin Qiao Yao Dong Hongli Zhou Hao Cui Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides Antibiotics polyene macrolides post-PKS modifications property antifungal activity |
title | Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides |
title_full | Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides |
title_fullStr | Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides |
title_full_unstemmed | Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides |
title_short | Effect of Post–Polyketide Synthase Modification Groups on Property and Activity of Polyene Macrolides |
title_sort | effect of post polyketide synthase modification groups on property and activity of polyene macrolides |
topic | polyene macrolides post-PKS modifications property antifungal activity |
url | https://www.mdpi.com/2079-6382/12/1/119 |
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