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| {{STRUCTURE_1llb| PDB=1llb | SCENE= }} | | {{STRUCTURE_1llb| PDB=1llb | SCENE= }} |
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| '''Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With ATMO-penicillin'''
| | ===Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With ATMO-penicillin=== |
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| ==Overview==
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| 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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_12323371}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 12323371 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_12323371}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Hydrolase]] | | [[Category: Hydrolase]] |
| [[Category: Serine]] | | [[Category: Serine]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:02:04 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 21:22:09 2008'' |
