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@ARTICLE{Vandavasi:280722,
author = {Vandavasi, Venu Gopal and Weiss, Kevin L. and Cooper,
Jonathan B. and Erskine, Peter T. and Tomanicek, Stephen J.
and Ostermann, Andreas and Schrader, Tobias E. and Ginell,
Stephan L. and Coates, Leighton},
title = {{E}xploring the {M}echanism of β-{L}actam {R}ing
{P}rotonation in the {C}lass {A} β-lactamase {A}cylation
{M}echanism {U}sing {N}eutron and {X}-ray {C}rystallography},
journal = {Journal of medicinal chemistry},
volume = {59},
issn = {1520-4804},
address = {Washington, DC},
publisher = {ACS},
reportid = {FZJ-2016-00479},
pages = {acs.jmedchem.5b01215},
year = {2015},
abstract = {The catalytic mechanism of class A β-lactamases is often
debated due in part to the large number of amino acids that
interact with bound β-lactam substrates. The role and
function of the conserved residue Lys 73 in the catalytic
mechanism of class A type β-lactamase enzymes is still not
well understood after decades of scientific research. To
better elucidate the functions of this vital residue, we
used both neutron and high-resolution X-ray diffraction to
examine both the structures of the ligand free protein and
the acyl–enzyme complex of perdeuterated E166A Toho-1
β-lactamase with the antibiotic cefotaxime. The E166A
mutant lacks a critical glutamate residue that has a key
role in the deacylation step of the catalytic mechanism,
allowing the acyl–enzyme adduct to be captured for study.
In our ligand free structures, Lys 73 is present in a single
conformation, however in all of our acyl–enzyme
structures, Lys 73 is present in two different
conformations, in which one conformer is closer to Ser 70
while the other conformer is positioned closer to Ser 130,
which supports the existence of a possible pathway by which
proton transfer from Lys 73 to Ser 130 can occur. This and
further clarifications of the role of Lys 73 in the
acylation mechanism may facilitate the design of inhibitors
that capitalize on the enzyme’s native machinery.},
cin = {JCNS (München) ; Jülich Centre for Neutron Science JCNS
(München) ; JCNS-FRM-II / Neutronenstreuung ; JCNS-1},
ddc = {540},
cid = {I:(DE-Juel1)JCNS-FRM-II-20110218 /
I:(DE-Juel1)JCNS-1-20110106},
pnm = {6G15 - FRM II / MLZ (POF3-6G15) / 6G4 - Jülich Centre for
Neutron Research (JCNS) (POF3-623)},
pid = {G:(DE-HGF)POF3-6G15 / G:(DE-HGF)POF3-6G4},
experiment = {EXP:(DE-MLZ)BIODIFF-20140101},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000368564400033},
pubmed = {pmid:26630115},
doi = {10.1021/acs.jmedchem.5b01215},
url = {https://juser.fz-juelich.de/record/280722},
}