Development of 6 '-N-Acylated Isepamicin Analogs with Improved Antibacterial Activity against Isepamicin-Resistant Pathogens
DC Field | Value | Language |
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dc.contributor.author | Ban, Yeon Hee | - |
dc.contributor.author | Song, Myoung Chong | - |
dc.contributor.author | Kim, Hee Jin | - |
dc.contributor.author | Lee, Heejeong | - |
dc.contributor.author | Wi, Jae Bok | - |
dc.contributor.author | Park, Je Won | - |
dc.contributor.author | Lee, Dong Gun | - |
dc.contributor.author | Yoon, Yeo Joon | - |
dc.date.accessioned | 2021-08-30T22:08:23Z | - |
dc.date.available | 2021-08-30T22:08:23Z | - |
dc.date.created | 2021-06-19 | - |
dc.date.issued | 2020-06 | - |
dc.identifier.issn | 2218-273X | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/55415 | - |
dc.description.abstract | The development of new aminoglycoside (AG) antibiotics has been required to overcome the resistance mechanism of AG-modifying enzymes (AMEs) of AG-resistant pathogens. The AG acetyltransferase, AAC(6')-APH(2 ''), one of the most typical AMEs, exhibiting substrate promiscuity towards a variety of AGs and acyl-CoAs, was employed to enzymatically synthesize new 6'-N-acylated isepamicin (ISP) analogs, 6'-N-acetyl/-propionyl/-malonyl ISPs. They were all active against the ISP-resistant Gram-negative bacteria tested, and the 6'-N-acetyl ISP displayed reduced toxicity compared to ISP in vitro. This study demonstrated the importance of the modification of the 6'-amino group in circumventing AG-resistance and the potential of regioselective enzymatic modification of AG scaffolds for the development of more robust AG antibiotics. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | MDPI | - |
dc.subject | AMINOGLYCOSIDE | - |
dc.subject | ANTIBIOTICS | - |
dc.subject | TOXICITY | - |
dc.subject | SIDE | - |
dc.title | Development of 6 '-N-Acylated Isepamicin Analogs with Improved Antibacterial Activity against Isepamicin-Resistant Pathogens | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Park, Je Won | - |
dc.identifier.doi | 10.3390/biom10060893 | - |
dc.identifier.scopusid | 2-s2.0-85086621908 | - |
dc.identifier.wosid | 000550892400001 | - |
dc.identifier.bibliographicCitation | BIOMOLECULES, v.10, no.6 | - |
dc.relation.isPartOf | BIOMOLECULES | - |
dc.citation.title | BIOMOLECULES | - |
dc.citation.volume | 10 | - |
dc.citation.number | 6 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.subject.keywordPlus | AMINOGLYCOSIDE | - |
dc.subject.keywordPlus | ANTIBIOTICS | - |
dc.subject.keywordPlus | TOXICITY | - |
dc.subject.keywordPlus | SIDE | - |
dc.subject.keywordAuthor | isepamicin analogs | - |
dc.subject.keywordAuthor | 6 &apos | - |
dc.subject.keywordAuthor | -N-acylation | - |
dc.subject.keywordAuthor | enzymatic synthesis | - |
dc.subject.keywordAuthor | antibacterial activity | - |
dc.subject.keywordAuthor | cytotoxicity | - |
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