| Title: |
Synthesis, mechanism of action, and SAR studies on the cyclic lipopeptide antibiotic daptomycin. |
| Authors: |
Taylor, Scott D.1 (AUTHOR) s5taylor@uwaterloo.ca |
| Source: |
Canadian Journal of Chemistry. 2024, Vol. 102 Issue 7, p414-424. 11p. |
| Subject Terms: |
*LIPOPEPTIDE antibiotics, *DAPTOMYCIN, *DRUG resistance in bacteria, *STRUCTURE-activity relationships, *PEPTIDE antibiotics, *GRAM-positive bacteria |
| Abstract: |
Daptomycin is a calcium-dependent cyclic lipopeptide antibiotic. It is one of only two new structural classes of antibiotics that have been approved for clinical use over the last 40 years. It is used to treat serious infections caused by Gram-positive bacteria. Although daptomycin has been used in the clinic since 2003, clinical resistance to daptomycin is not yet widespread. However, reports of clinical isolates that are resistant to daptomycin have been increasing in recent years, which is a cause for concern since daptomycin is often used to treat serious infections that are resistant to other antibiotics. Structural variation of antibiotics is a strategy that has often been used to overcome bacterial resistance. To pursue such a strategy with daptomycin, knowledge of its mechanism of action and methods for preparing daptomycin analogues, and the development of daptomycin structure–activity relationships (SARs) are necessary. This article, which is based on the 2023 Bernard Belleau Award Lecture, provides an overview of some of the key investigations that were undertaken by the Taylor group on daptomycin, including mechanism of action studies, the total synthesis of daptomycin, daptomycin SARs, and characterization of the interaction of daptomycin with phosphatidylglycerol, its primary target. [ABSTRACT FROM AUTHOR] |
|
Copyright of Canadian Journal of Chemistry is the property of Canadian Science Publishing and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) |
| Database: |
Academic Search Complete |
