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A High-Resolution Crystal Structure that Reveals Molecular Details of Target Recognition by the Calcium-Dependent Lipopeptide Antibiotic Laspartomycin C.

ABSTRACT: The calcium-dependent antibiotics (CDAs) are an important emerging class of antibiotics. The crystal structure of the CDA laspartomycin C in complex with calcium and the ligand geranyl-phosphate at a resolution of 1.28 Å is reported. This is the first crystal structure of a CDA bound to its bacterial target. The structure is also the first to be reported for an antibiotic that binds the essential bacterial phospholipid undecaprenyl phosphate (C₅₅ -P). These structural insights are of great value in the design of antibiotics capable of exploiting this unique bacterial target.

SUBMITTER: Kleijn LHJ

PROVIDER: S-EPMC5767759 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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A High-Resolution Crystal Structure that Reveals Molecular Details of Target Recognition by the Calcium-Dependent Lipopeptide Antibiotic Laspartomycin C.

Kleijn Laurens H J LHJ Vlieg Hedwich C HC Wood Thomas M TM Sastre Toraño Javier J Janssen Bert J C BJC Martin Nathaniel I NI

Angewandte Chemie (International ed. in English) 20171130 52

The calcium-dependent antibiotics (CDAs) are an important emerging class of antibiotics. The crystal structure of the CDA laspartomycin C in complex with calcium and the ligand geranyl-phosphate at a resolution of 1.28 Å is reported. This is the first crystal structure of a CDA bound to its bacterial target. The structure is also the first to be reported for an antibiotic that binds the essential bacterial phospholipid undecaprenyl phosphate (C<sub>55</sub> -P). These structural insights are of ...[more]

PMID: 29108098

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