Dynamic combinatorial mass spectrometry leads to metallo-beta-lactamase inhibitors.

Kinetics; Models, Molecular; Spectrometry, Mass, Electrospray Ionization; Structure-Activity Relationship; Sulfhydryl Compounds/chemical synthesis/chemistry; beta-Lactamase Inhibitors; beta-Lactamases/chemistry

Abstract :

[en] The use of protein ESI mass spectrometry under non-denaturing conditions to analyze a dynamic combinatorial library of thiols/disulfides with the BcII metallo-beta-lactamase enabled the rapid identification of an inhibitor with a K(i) of < 1 microM. The study exemplifies the utility of protein-MS for screening dynamic mixtures of potential enzyme-inhibitors.

Disciplines :

Biochemistry, biophysics & molecular biology

Author, co-author :

Lienard, Benoit M. R.

Huting, Rebekka

Lassaux, Patricia ; Université de Liège - ULiège > GIGA-R : Virologie - Immunologie

Galleni, Moreno ; Université de Liège - ULiège > Département des sciences de la vie > Macromolécules biologiques

Frère, Jean-Marie ; Université de Liège - ULiège > Centre d'ingénierie des protéines

Schofield, Christopher J.

Language :

English

Title :

Dynamic combinatorial mass spectrometry leads to metallo-beta-lactamase inhibitors.

Publication date :

2008

Journal title :

Journal of Medicinal Chemistry

ISSN :

0022-2623

eISSN :

1520-4804

Publisher :

American Chemical Society, Washington, United States - District of Columbia

Volume :

Issue :

Pages :

684-8

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 22 December 2014

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Bibliography

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