TY - JOUR
T1 - Crystal structure of Enterobacter cloacae 908R class C β-lactamase bound to iodo-acetamido-phenyl boronic acid, a transition-state analogue
AU - Wouters, J.
AU - Fonzé, E.
AU - Vermeire, M.
AU - Frère, J. M.
AU - Charlier, P.
PY - 2003/8/1
Y1 - 2003/8/1
N2 - The structures of the class C β-lactamase from Enterobacter cloacae 908R alone and in complex with a boronic acid transition-state analogue were determined by X-ray crystallography at 2.1 and 2.3 Å, respectively. The structure of the enzyme resembles those of other class C β-lactamases. The structure of the complex with the transition-state analogue, iodo-acetamido-phenyl boronic acid, shows that the inhibitor is covalently bound to the active-site serine (Ser64). Binding of the inhibitor within the active site is compared with previously determined structures of complexes with other class C enzymes. The structure of the boronic acid adduct indicates ways to improve the affinity of this class of inhibitors. This structure of 908R class C β-lactamase in complex with a transition-state analogue provides further insights into the mechanism of action of these hydrolases.
AB - The structures of the class C β-lactamase from Enterobacter cloacae 908R alone and in complex with a boronic acid transition-state analogue were determined by X-ray crystallography at 2.1 and 2.3 Å, respectively. The structure of the enzyme resembles those of other class C β-lactamases. The structure of the complex with the transition-state analogue, iodo-acetamido-phenyl boronic acid, shows that the inhibitor is covalently bound to the active-site serine (Ser64). Binding of the inhibitor within the active site is compared with previously determined structures of complexes with other class C enzymes. The structure of the boronic acid adduct indicates ways to improve the affinity of this class of inhibitors. This structure of 908R class C β-lactamase in complex with a transition-state analogue provides further insights into the mechanism of action of these hydrolases.
KW - Boronic acid complex
KW - Class-C β-lactamase
KW - Enterobacter cloacae 908R
KW - Iodo-acetamido-phenyl boronic acid (IAPB)
KW - Transition-state analogue
UR - http://www.scopus.com/inward/record.url?scp=0042830810&partnerID=8YFLogxK
U2 - 10.1007/s00018-003-3189-2
DO - 10.1007/s00018-003-3189-2
M3 - Article
C2 - 14521155
AN - SCOPUS:0042830810
SN - 1420-682X
VL - 60
SP - 1764
EP - 1773
JO - Cellular and Molecular Life Sciences
JF - Cellular and Molecular Life Sciences
IS - 8
ER -