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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Main Authors: Liqin Qiao, Yao Dong, Hongli Zhou, Hao Cui
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:Antibiotics
Subjects:
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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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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