[en] Following from the evaluation of different types of electrophiles, combined modeling and
crystallographic analyses are used to generate potent boronic acid based inhibitors of a penicillin binding
protein. The results suggest that a structurally informed approach to penicillin binding protein inhibition
will be useful for the development of both improved reversibly binding inhibitors, including boronic acids,
and acylating inhibitors, such as β-lactams.
Disciplines :
Biochemistry, biophysics & molecular biology
Author, co-author :
Woon, Esther C. Y.
Zervosen, Astrid ; Université de Liège - ULiège > Centre de recherches du cyclotron
Sauvage, Eric ; Université de Liège - ULiège > Centre d'ingénierie des protéines
Simmons, Katie J.
Zivec, Matej
Inglis, Steven R.
Fishwick, Colin W. G.
Gobec, Stanislav
Charlier, Paulette ; Université de Liège - ULiège > Département des sciences de la vie > Cristallographie des macromolécules biologiques
Luxen, André ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse
Schofield, Christopher J.
Language :
English
Title :
Structure Guided Development of Potent Reversibly Binding Penicillin Binding Protein Inhibitors
Publication date :
2011
Journal title :
ACS Medicinal Chemistry Letters
eISSN :
1948-5875
Publisher :
American Chemical Society, Washington, United States - District of Columbia
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