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Article: Establishing the structure-activity relationship of teixobactin

TitleEstablishing the structure-activity relationship of teixobactin
Authors
KeywordsTeixobactin
Antibacterial
Peptide synthesis
Structure-activity relationship
Cyclic peptides
Issue Date2019
PublisherElsevier Ltd for Chinese Chemical Society. The Journal's web site is located at http://www.chinchemlett.com.cn
Citation
Chinese Chemical Letters, 2019, v. 30 n. 8, p. 1468-1480 How to Cite?
AbstractIn 2015, a new antimicrobial peptide agent was discovered, termed teixobactin. Over the past few years, the structure-activity relationship of teixobactin has been extensively studied. Here, the updated studies have been summarized to provide structure-activity relationship established to date. It can be seen that position 1, 2, 5 and 6 of teixobactin are not tolerant of diversion from the native amino acids. In positions 7 and 11, native amino acids give the highest activity but there is tolerance for other amino acids. Positions 3, 4, 9 and 10 are very tolerant of substitution while maintaining good potency and a broad activity spectrum. Activity does not depend on absolute stereochemistry, but on the relative stereochemistry and positions 1, 4, 5, and 8 must contain d-amino acids. The ring and tail structure are necessary for activity, macrolactone and lactam rings are both acceptable. Some teixobactin analogues show greater activity than native teixobactin. All conducted animal studies show positive results with no animal deaths.
Persistent Identifierhttp://hdl.handle.net/10722/284530
ISSN
2019 Impact Factor: 4.632
2015 SCImago Journal Rankings: 0.451
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorMatheson, E-
dc.contributor.authorJIN, K-
dc.contributor.authorLi, X-
dc.date.accessioned2020-08-07T08:58:57Z-
dc.date.available2020-08-07T08:58:57Z-
dc.date.issued2019-
dc.identifier.citationChinese Chemical Letters, 2019, v. 30 n. 8, p. 1468-1480-
dc.identifier.issn1001-8417-
dc.identifier.urihttp://hdl.handle.net/10722/284530-
dc.description.abstractIn 2015, a new antimicrobial peptide agent was discovered, termed teixobactin. Over the past few years, the structure-activity relationship of teixobactin has been extensively studied. Here, the updated studies have been summarized to provide structure-activity relationship established to date. It can be seen that position 1, 2, 5 and 6 of teixobactin are not tolerant of diversion from the native amino acids. In positions 7 and 11, native amino acids give the highest activity but there is tolerance for other amino acids. Positions 3, 4, 9 and 10 are very tolerant of substitution while maintaining good potency and a broad activity spectrum. Activity does not depend on absolute stereochemistry, but on the relative stereochemistry and positions 1, 4, 5, and 8 must contain d-amino acids. The ring and tail structure are necessary for activity, macrolactone and lactam rings are both acceptable. Some teixobactin analogues show greater activity than native teixobactin. All conducted animal studies show positive results with no animal deaths.-
dc.languageeng-
dc.publisherElsevier Ltd for Chinese Chemical Society. The Journal's web site is located at http://www.chinchemlett.com.cn-
dc.relation.ispartofChinese Chemical Letters-
dc.subjectTeixobactin-
dc.subjectAntibacterial-
dc.subjectPeptide synthesis-
dc.subjectStructure-activity relationship-
dc.subjectCyclic peptides-
dc.titleEstablishing the structure-activity relationship of teixobactin-
dc.typeArticle-
dc.identifier.emailLi, X: xuechenl@hku.hk-
dc.identifier.authorityLi, X=rp00742-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.cclet.2019.07.004-
dc.identifier.scopuseid_2-s2.0-85069575632-
dc.identifier.hkuros311892-
dc.identifier.volume30-
dc.identifier.issue8-
dc.identifier.spage1468-
dc.identifier.epage1480-
dc.identifier.isiWOS:000482249800003-
dc.publisher.placeChina-
dc.identifier.issnl1001-8417-

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