Article (Scientific journals)
Dynamic combinatorial mass spectrometry leads to metallo-beta-lactamase inhibitors.
Lienard, Benoit M. R.; Huting, Rebekka; Lassaux, Patricia et al.
2008In Journal of Medicinal Chemistry, 51 (3), p. 684-8
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Keywords :
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 :
51
Issue :
3
Pages :
684-8
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 22 December 2014

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