2p9v: Difference between revisions

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caption="2p9v, resolution 1.80Å" />

'''Structure of AmpC beta-lactamase with cross-linked active site after exposure to small molecule inhibitor'''<br />

~~==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==

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==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17628063 17628063]

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: Escherichia coli]]

[[Category: Protein complex]]

[[Category: Babaoglu, K.]]

[[Category: Pelto, R.B.]]

[[Category: Pelto, R B.]]

[[Category: Pratt, R.F.]]

[[Category: Pratt, R F.]]

[[Category: Shoichet, B.K.]]

[[Category: Shoichet, B K.]]

[[Category: Wyrembak, P.N.]]

[[Category: Wyrembak, P N.]]

[[Category: PO4]]

[[Category: beta-lactamase]]

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[[Category: hydrolase]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:27:30 2008''

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@@ Line 2: / Line 2: @@
 caption="2p9v, resolution 1.80&Aring;" />
 '''Structure of AmpC beta-lactamase with cross-linked active site after exposure to small molecule inhibitor'''<br />
-==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==
@@ Line 10: / Line 7: @@
 ==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17628063 17628063]
+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: Escherichia coli]]
 [[Category: Protein complex]]
 [[Category: Babaoglu, K.]]
-[[Category: Pelto, R.B.]]
+[[Category: Pelto, R B.]]
-[[Category: Pratt, R.F.]]
+[[Category: Pratt, R F.]]
-[[Category: Shoichet, B.K.]]
+[[Category: Shoichet, B K.]]
-[[Category: Wyrembak, P.N.]]
+[[Category: Wyrembak, P N.]]
 [[Category: PO4]]
 [[Category: beta-lactamase]]
@@ Line 24: / Line 21: @@
 [[Category: hydrolase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:12:46 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:27:30 2008''