1llb

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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'''
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===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.
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(as it appears on PubMed at http://www.pubmed.gov), where 12323371 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12323371}}
==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Serine]]
[[Category: Serine]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:02:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 21:22:09 2008''

Revision as of 18:22, 2 July 2008

Image:1llb.png

Template:STRUCTURE 1llb

Crystal Structure Of AmpC beta-Lactamase From E. Coli In Complex With ATMO-penicillin

Template:ABSTRACT PUBMED 12323371

About this Structure

1LLB is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

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

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