2rcx: Difference between revisions

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[[Image:2rcx.~~gif~~|left|200px]]

[[Image:2rcx.png|left|200px]]

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~~'''~~AmpC Beta-lactamase in complex with (1R)-1-(2-Thiophen-2-yl-acetylamino)-1-(3-(2-carboxyvinyl)-phenyl) methylboronic acid~~'''~~

===AmpC Beta-lactamase in complex with (1R)-1-(2-Thiophen-2-yl-acetylamino)-1-(3-(2-carboxyvinyl)-phenyl) methylboronic acid===

~~==Overview==~~

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~~Boronic acids have proved to be promising selective inhibitors of beta~~-~~lactamases, acting as transition state analogues. Starting from a previously described nanomolar inhibitor of AmpC beta~~-~~lactamase~~, ~~three new inhibitors were designed to gain interactions with highly conserved residues~~, ~~such as Asn343, and to bind more tightly~~ to the ~~enzyme. Among these, one was obtained by stereoselective synthesis and succeeded in placing its anionic group into the carboxylate binding site of the enzyme,~~ as ~~revealed by X-ray crystallography of the complex inhibitor~~/~~AmpC~~. ~~Nevertheless, it failed at improving affinity~~, ~~when compared to~~ the ~~lead from which it was derived. The origins of this structural and energetic discrepancy are discussed~~.

The line below this paragraph, {{ABSTRACT_PUBMED_17997318}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 17997318 is the PubMed ID number.

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==About this Structure==

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[[Category: Periplasm]]

[[Category: Serine hydrolase]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sun May 4~~ 16:39:30 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:11:55 2008''

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-[[Image:2rcx.gif|left|200px]]
+{{Seed}}
+[[Image:2rcx.png|left|200px]]
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 {{STRUCTURE_2rcx|  PDB=2rcx  |  SCENE=  }}
-'''AmpC Beta-lactamase in complex with (1R)-1-(2-Thiophen-2-yl-acetylamino)-1-(3-(2-carboxyvinyl)-phenyl) methylboronic acid'''
+===AmpC Beta-lactamase in complex with (1R)-1-(2-Thiophen-2-yl-acetylamino)-1-(3-(2-carboxyvinyl)-phenyl) methylboronic acid===
-==Overview==
+<!--
-Boronic acids have proved to be promising selective inhibitors of beta-lactamases, acting as transition state analogues. Starting from a previously described nanomolar inhibitor of AmpC beta-lactamase, three new inhibitors were designed to gain interactions with highly conserved residues, such as Asn343, and to bind more tightly to the enzyme. Among these, one was obtained by stereoselective synthesis and succeeded in placing its anionic group into the carboxylate binding site of the enzyme, as revealed by X-ray crystallography of the complex inhibitor/AmpC. Nevertheless, it failed at improving affinity, when compared to the lead from which it was derived. The origins of this structural and energetic discrepancy are discussed.
+The line below this paragraph, {{ABSTRACT_PUBMED_17997318}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 17997318 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_17997318}}
 ==About this Structure==
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 [[Category: Periplasm]]
 [[Category: Serine hydrolase]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 16:39:30 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:11:55 2008''