Structure Guided Development of Potent Reversibly Binding Penicillin Binding Protein Inhibitors

[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

Volume :

2 (3)

Pages :

219-223

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 28 July 2011

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Bibliography

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