2p9v
From Proteopedia
(Difference between revisions)
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caption="2p9v, resolution 1.80Å" /> | caption="2p9v, resolution 1.80Å" /> | ||
'''Structure of AmpC beta-lactamase with cross-linked active site after exposure to small molecule inhibitor'''<br /> | '''Structure of AmpC beta-lactamase with cross-linked active site after exposure to small molecule inhibitor'''<br /> | ||
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| - | ==Overview== | ||
| - | O-Aryloxycarbonyl hydroxamates represent a new class of beta-lactamase, inhibitors. N-Benzyloxycarbonyl-O-(phenoxycarbonyl) hydroxylamine, for, example, inactivates the class C Enterobacter cloacae P99 beta-lactamase, with a rate constant of 6.1 x 103 s-1 M-1; approximately two turnover, events accompany the inhibition., N-Benzyloxycarbonyl-O-[(3-carboxyphenoxy)carbonyl] hydroxylamine is, comparably effective. These compounds also inactivate the class A TEM, beta-lactamase. A crystal structure of the inactivated AmpC enzyme, another class C beta-lactamase, reveals that the active site has become, cross-linked by a carbamate bridge spanning Ser64, the active site, nucleophile, and Lys315, a conserved active site residue. | ||
==About this Structure== | ==About this Structure== | ||
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==Reference== | ==Reference== | ||
| - | O- | + | O-aryloxycarbonyl hydroxamates: new beta-lactamase inhibitors that cross-link the active site., Wyrembak PN, Babaoglu K, Pelto RB, Shoichet BK, Pratt RF, J Am Chem Soc. 2007 Aug 8;129(31):9548-9. Epub 2007 Jul 12. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17628063 17628063] |
[[Category: Beta-lactamase]] | [[Category: Beta-lactamase]] | ||
[[Category: Escherichia coli]] | [[Category: Escherichia coli]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Babaoglu, K.]] | [[Category: Babaoglu, K.]] | ||
| - | [[Category: Pelto, R | + | [[Category: Pelto, R B.]] |
| - | [[Category: Pratt, R | + | [[Category: Pratt, R F.]] |
| - | [[Category: Shoichet, B | + | [[Category: Shoichet, B K.]] |
| - | [[Category: Wyrembak, P | + | [[Category: Wyrembak, P N.]] |
[[Category: PO4]] | [[Category: PO4]] | ||
[[Category: beta-lactamase]] | [[Category: beta-lactamase]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:27:30 2008'' |
Revision as of 16:27, 21 February 2008
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Structure of AmpC beta-lactamase with cross-linked active site after exposure to small molecule inhibitor
About this Structure
2P9V is a Protein complex structure of sequences from Escherichia coli with as ligand. Active as Beta-lactamase, with EC number 3.5.2.6 Full crystallographic information is available from OCA.
Reference
O-aryloxycarbonyl hydroxamates: new beta-lactamase inhibitors that cross-link the active site., Wyrembak PN, Babaoglu K, Pelto RB, Shoichet BK, Pratt RF, J Am Chem Soc. 2007 Aug 8;129(31):9548-9. Epub 2007 Jul 12. PMID:17628063
Page seeded by OCA on Thu Feb 21 18:27:30 2008
