[en] Lactivicin (LTV) is a natural non-beta-lactam antibiotic that inhibits penicillin-binding proteins and serine beta-lactamases. A crystal structure of a BS3-LTV complex reveals that, as for its reaction with PBPs, LTV reacts with the nucleophilic serine and that cycloserine and lactone rings of LTV are opened. This structure, together with reported structures of PBP1b with lactivicins, provides a basis for developing improved lactivicin-based gamma-lactam antibiotics.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Brown, Tom Jr
Charlier, Paulette ; Université de Liège - ULiège > Département des sciences de la vie > Cristallographie des macromolécules biologiques
Herman, Raphaël ; Université de Liège - ULiège > Centre d'ingénierie des protéines
Schofield, Christopher J
Sauvage, Eric ; Université de Liège - ULiège > Centre d'ingénierie des protéines
Language :
English
Title :
Structural basis for the interaction of lactivicins with serine beta-lactamases.
Publication date :
2010
Journal title :
Journal of Medicinal Chemistry
ISSN :
0022-2623
eISSN :
1520-4804
Publisher :
American Chemical Society, Washington, United States - District of Columbia
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