Citation: Matheson Eilidh, Jin Kang, Li Xuechen. Establishing the structure-activity relationship of teixobactin[J]. Chinese Chemical Letters, ;2019, 30(8): 1468-1480. doi: 10.1016/j.cclet.2019.07.004 shu

Establishing the structure-activity relationship of teixobactin

Matheson Eilidh ^c ,
Jin Kang ^a ,
Li Xuechen ^a,b,*,

a.
Department of Chemistry, State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong, China
b.
Laboratory of Marine Drugs and Bioprodcuts, Qingdao National Laboratory for Marine Science and Technology, Qingdao 266237, China
c.
School of Chemistry, University of Edinburgh, Edinburgh, UK

xuechenl@hku.hk

Received Date: 25 May 2019
Revised Date: 14 June 2019
Accepted Date: 1 July 2019
Available Online: 2 August 2019

Figures(15)

In 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.
- Teixobactin,
- Antibacterial,
- Peptide synthesis,
- Structure-activity relationship,
- Cyclic peptides
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