3tsg: Difference between revisions
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==Crystal structure of GES-14== | |||
=== | <StructureSection load='3tsg' size='340' side='right' caption='[[3tsg]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3tsg]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Acinetobacter_baumannii Acinetobacter baumannii]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3TSG OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3TSG FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2qpn|2qpn]]</td></tr> | |||
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">blaGES-14 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=470 Acinetobacter baumannii])</td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Beta-lactamase Beta-lactamase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.2.6 3.5.2.6] </span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3tsg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3tsg OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3tsg RCSB], [http://www.ebi.ac.uk/pdbsum/3tsg PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
GES-1 is a class A extended-spectrum beta-lactamase conferring resistance to penicillins, first-, second-generation cephalosporins and to ceftazidime. However, GES-1 poorly hydrolyzes aztreonam and cephamycins, and exhibits very low k(cat) values for carbapenems. Twenty-two GES variants have been discovered thus far, differing from each other by 1-3 amino acid substitutions that affect substrate specificity. GES-11 possesses a Gly243Ala substitution which seems to confer this variant an increased activity against aztreonam and ceftazidime. GES-12 differs from GES-11 by a single Thr237Ala substitution while GES-14 differs from GES-11 by the Gly170Ser mutation which is known to confer increased carbapenemase activity. GES-11 and GES-12 were kinetically characterized and compared with GES-1 and GES-14. Purified GES-11 and GES-12 showed strong activities against most tested beta-lactams with the exception of temocillin, cefoxitin and carbapenems. Both variants showed a significantly increased rate of hydrolysis of cefotaxime, ceftazidime and aztreonam. On the other hand, GES-11, GES-12 (and GES-14) variants all containing Ala243 exhibited increased susceptibility to classical inhibitors. The crystallographic structures of the GES-11 and GES-14 beta-lactamases were solved. The overall structures of GES-11 and GES-14 are similar to that of GES-1. The Gly243Ala substitution caused only subtle local rearrangements, notably in the typical carbapenemase disulfide bond. The active sites of GES-14 and GES-11 are very similar, the Gly170Ser substitution leading only to the formation of additional hydrogen bonds of the Ser residue with the hydrolytic water and the Glu166 residue. | |||
Kinetic and crystallographic studies of extended spectrum GES-11, GES-12 and GES-14 beta-lactamases.,Delbruck H, Bogaerts P, Kupper MB, de Castro RR, Bennink S, Glupczynski Y, Galleni M, Hoffmann KM, Bebrone C Antimicrob Agents Chemother. 2012 Aug 20. PMID:22908160<ref>PMID:22908160</ref> | |||
== | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | |||
==See Also== | |||
*[[Beta-lactamase|Beta-lactamase]] | |||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Acinetobacter baumannii]] | [[Category: Acinetobacter baumannii]] | ||
[[Category: Beta-lactamase]] | [[Category: Beta-lactamase]] | ||
[[Category: Bebrone, C | [[Category: Bebrone, C]] | ||
[[Category: Delbruck, H | [[Category: Delbruck, H]] | ||
[[Category: Hoffmann, K M.V | [[Category: Hoffmann, K M.V]] | ||
[[Category: Beta lactamase fold]] | [[Category: Beta lactamase fold]] | ||
[[Category: Beta lactam]] | [[Category: Beta lactam]] | ||
[[Category: Hydrolase]] | [[Category: Hydrolase]] | ||
