1ll9: Difference between revisions
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'''Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With Amoxicillin''' | '''Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With Amoxicillin''' | ||
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[[Category: Shoichet, B K.]] | [[Category: Shoichet, B K.]] | ||
[[Category: Trehan, I.]] | [[Category: Trehan, I.]] | ||
[[Category: | [[Category: Beta-lactamase]] | ||
[[Category: | [[Category: Cephalosporinase]] | ||
[[Category: | [[Category: Hydrolase]] | ||
[[Category: | [[Category: Serine]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:01:52 2008'' | |||
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Revision as of 00:01, 3 May 2008
Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With Amoxicillin
OverviewOverview
beta-lactamases confer resistance to beta-lactam antibiotics such as penicillins and cephalosporins. However, beta-lactams that form an acyl-intermediate with the enzyme but subsequently are hindered from forming a catalytically competent conformation seem to be inhibitors of beta-lactamases. This inhibition may be imparted by specific groups on the ubiquitous R(1) side chain of beta-lactams, such as the 2-amino-4-thiazolyl methoxyimino (ATMO) group common among third-generation cephalosporins. Using steric hindrance of deacylation as a design guide, penicillin and carbacephem substrates were converted into effective beta-lactamase inhibitors and antiresistance antibiotics. To investigate the structural bases of inhibition, the crystal structures of the acyl-adducts of the penicillin substrate amoxicillin and the new analogous inhibitor ATMO-penicillin were determined. ATMO-penicillin binds in a catalytically incompetent conformation resembling that adopted by third-generation cephalosporins, demonstrating the transferability of such sterically hindered groups in inhibitor design.
About this StructureAbout this Structure
1LL9 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.
ReferenceReference
Using steric hindrance to design new inhibitors of class C beta-lactamases., Trehan I, Morandi F, Blaszczak LC, Shoichet BK, Chem Biol. 2002 Sep;9(9):971-80. PMID:12323371 Page seeded by OCA on Sat May 3 00:01:52 2008