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A High‐Resolution Crystal Structure that Reveals Molecular Details of Target Recognition by the Calcium‐Dependent Lipopeptide Antibiotic Laspartomycin C
Author(s) -
Kleijn Laurens H. J.,
Vlieg Hedwich C.,
Wood Thomas M.,
Sastre Toraño Javier,
Janssen Bert J. C.,
Martin Nathaniel I.
Publication year - 2017
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201709240
Subject(s) - lipopeptide , antibiotics , chemistry , calcium , ligand (biochemistry) , resolution (logic) , stereochemistry , biochemistry , bacteria , biology , receptor , genetics , organic chemistry , artificial intelligence , computer science
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 55 ‐P). These structural insights are of great value in the design of antibiotics capable of exploiting this unique bacterial target.