ORBi: Beck Josephine - 2-Aminopropane-1,2,3-tricarboxylic acid: Synthesis and co-crystallization with the class A beta-lactamase BS3 of Bacillus licheniformis.

Reference : 2-Aminopropane-1,2,3-tricarboxylic acid: Synthesis and co-crystallization with the class...


	Document type :	Scientific journals : Article
	Discipline(s) :	Life sciences : Biochemistry, biophysics & molecular biology
	To cite this reference:	http://hdl.handle.net/2268/77965

Title :	2-Aminopropane-1,2,3-tricarboxylic acid: Synthesis and co-crystallization with the class A beta-lactamase BS3 of Bacillus licheniformis.
Language :	English
Author, co-author :	Beck, Josephine [> > > >]
	Sauvage, Eric [Université de Liège - ULg > > Centre d'ingénierie des protéines >]
	Charlier, Paulette [Université de Liège - ULg > Département des sciences de la vie > Cristallographie des macromolécules biologiques >]
	Marchand-Brynaert, Jacqueline [> > > >]
Publication date :	2008
Journal title :	Bioorganic & Medicinal Chemistry Letters
Publisher :	Elsevier Science
Volume :	18
Issue/season :	13
Pages :	3764-8
Audience :	International
ISSN :	0960-894X
e-ISSN :	1464-3405
City :	Oxford
Country :	United Kingdom
Keywords :	[en] Aspartic Acid/analogs & derivatives/chemical synthesis/chemistry ; Bacillus/enzymology/metabolism ; Bacterial Proteins/chemistry ; Binding Sites ; Cations ; Chemistry, Pharmaceutical/methods ; Citric Acid/chemistry ; Crystallography, X-Ray/methods ; Drug Design ; Isocitrates/chemistry ; Models, Chemical ; Molecular Conformation ; Oxygen/chemistry ; Tricarboxylic Acids/chemistry ; X-Ray Diffraction ; beta-Lactamases/metabolism
Abstract :	[en] The title compound 4 has been prepared in four steps from ethylglycinate in 63% overall yield. This amino analog of citric acid has been co-crystallized with the class A beta-lactamase BS3 of Bacillus licheniformis and the structure of the complex fully analyzed by X-ray diffraction. Tris-ethyl aminocitrate 3 and the free tris-acid 4 have been tested against a member beta-lactamase from all distinct subgroups. They are novel inhibitors of class A beta-lactamases, still modest but more potent than citrate and isocitrate.
Permalink :	http://hdl.handle.net/2268/77965
DOI :	10.1016/j.bmcl.2008.05.045

File(s) associated to this reference

Fulltext file(s):

	File	Commentary	Version	Size	Access
Open access	Beck_2008.pdf		Publisher postprint	399.28 kB	View/Open

All documents in ORBi are protected by a user license.

Dspace v1.5