Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities
- Author
- Anish Parmar, Stephen H Prior, Abhishek Iyer (UGent) , Charlotte S Vincent, Dorien Van Lysebetten, Eefjan Breukink, Annemieke Madder (UGent) , Edward J Taylor and Ishwar Singh
- Organization
- Abstract
- The discovery of the highly potent antibiotic teixobactin, which kills the bacteria without any detectable resistance, has stimulated interest in its structure-activity relationship. However, a molecular structure-activity relationship has not been established so far for teixobactin. Moreover, the importance of the individual amino acids in terms of their (L/D) configuration and their contribution to the molecular structure and biological activity are still unknown. For the first time, we have defined the molecular structure of seven teixobactin analogues through the variation of the (D/L) configuration of its key residues, namely N-Me-(D)-Phe, (D)-Gln, (D)-allo-Ile and (D)-Thr. Furthermore, we have established the role of the individual (D) amino acids and correlated this with the molecular structure and biological activity. Through extensive NMR and structural calculations, including molecular dynamics simulations, we have revealed the residues for maintaining a reasonably unstructured teixobactin which is imperative for biological activity.
- Keywords
- SUBSTITUTION
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Citation
Please use this url to cite or link to this publication: http://hdl.handle.net/1854/LU-8506496
- MLA
- Parmar, Anish, et al. “Defining the Molecular Structure of Teixobactin Analogues and Understanding Their Role in Antibacterial Activities.” CHEMICAL COMMUNICATIONS, vol. 53, no. 12, 2017, pp. 2016–19, doi:10.1039/c6cc09490b.
- APA
- Parmar, A., Prior, S. H., Iyer, A., Vincent, C. S., Van Lysebetten, D., Breukink, E., … Singh, I. (2017). Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities. CHEMICAL COMMUNICATIONS, 53(12), 2016–2019. https://doi.org/10.1039/c6cc09490b
- Chicago author-date
- Parmar, Anish, Stephen H Prior, Abhishek Iyer, Charlotte S Vincent, Dorien Van Lysebetten, Eefjan Breukink, Annemieke Madder, Edward J Taylor, and Ishwar Singh. 2017. “Defining the Molecular Structure of Teixobactin Analogues and Understanding Their Role in Antibacterial Activities.” CHEMICAL COMMUNICATIONS 53 (12): 2016–19. https://doi.org/10.1039/c6cc09490b.
- Chicago author-date (all authors)
- Parmar, Anish, Stephen H Prior, Abhishek Iyer, Charlotte S Vincent, Dorien Van Lysebetten, Eefjan Breukink, Annemieke Madder, Edward J Taylor, and Ishwar Singh. 2017. “Defining the Molecular Structure of Teixobactin Analogues and Understanding Their Role in Antibacterial Activities.” CHEMICAL COMMUNICATIONS 53 (12): 2016–2019. doi:10.1039/c6cc09490b.
- Vancouver
- 1.Parmar A, Prior SH, Iyer A, Vincent CS, Van Lysebetten D, Breukink E, et al. Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities. CHEMICAL COMMUNICATIONS. 2017;53(12):2016–9.
- IEEE
- [1]A. Parmar et al., “Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities,” CHEMICAL COMMUNICATIONS, vol. 53, no. 12, pp. 2016–2019, 2017.
@article{8506496, abstract = {{The discovery of the highly potent antibiotic teixobactin, which kills the bacteria without any detectable resistance, has stimulated interest in its structure-activity relationship. However, a molecular structure-activity relationship has not been established so far for teixobactin. Moreover, the importance of the individual amino acids in terms of their (L/D) configuration and their contribution to the molecular structure and biological activity are still unknown. For the first time, we have defined the molecular structure of seven teixobactin analogues through the variation of the (D/L) configuration of its key residues, namely N-Me-(D)-Phe, (D)-Gln, (D)-allo-Ile and (D)-Thr. Furthermore, we have established the role of the individual (D) amino acids and correlated this with the molecular structure and biological activity. Through extensive NMR and structural calculations, including molecular dynamics simulations, we have revealed the residues for maintaining a reasonably unstructured teixobactin which is imperative for biological activity.}}, author = {{Parmar, Anish and Prior, Stephen H and Iyer, Abhishek and Vincent, Charlotte S and Van Lysebetten, Dorien and Breukink, Eefjan and Madder, Annemieke and Taylor, Edward J and Singh, Ishwar}}, issn = {{1359-7345}}, journal = {{CHEMICAL COMMUNICATIONS}}, keywords = {{SUBSTITUTION}}, language = {{eng}}, number = {{12}}, pages = {{2016--2019}}, title = {{Defining the molecular structure of teixobactin analogues and understanding their role in antibacterial activities}}, url = {{http://doi.org/10.1039/c6cc09490b}}, volume = {{53}}, year = {{2017}}, }
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