2i72

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{{STRUCTURE_2i72| PDB=2i72 | SCENE= }}
{{STRUCTURE_2i72| PDB=2i72 | SCENE= }}
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'''AmpC beta-lactamase in complex with 5-diformylaminomethyl-benzo[b]thiophen-2-boronic acid'''
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===AmpC beta-lactamase in complex with 5-diformylaminomethyl-benzo[b]thiophen-2-boronic acid===
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==Overview==
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Benzo[b]thiophene-2-ylboronic acid, 1, is a 27 nM inhibitor of the class C beta-lactamase AmpC and potentiates the activity of beta-lactam antibiotics in bacteria that express this and related enzymes. As is often true, the potency of compound 1 against the enzymes is much attenuated in cell culture against Gram negative bacteria, where the minimum inhibitor concentration of compound 1 is in the mid-micromolar range. Here, we modulated the properties of this lead to enhance its ability to cross the membrane, using a combination of X-ray crystallography, structure-based design, and application of physical models of outer membrane crossing. This strategy led us to derivatives with substantially improved permeability. Also, the greater solubility of these compounds allowed us to measure their efficacy at higher concentrations than with the lead 1, leading to higher maximum potentiation of the antibiotic effect of ceftazidime on resistant bacteria.
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(as it appears on PubMed at http://www.pubmed.gov), where 17956081 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17956081}}
==About this Structure==
==About this Structure==
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[[Category: Cephalosporinase]]
[[Category: Cephalosporinase]]
[[Category: Serine hydrolase]]
[[Category: Serine hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:09:38 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 04:15:01 2008''

Revision as of 01:15, 29 July 2008

Image:2i72.png

Template:STRUCTURE 2i72

AmpC beta-lactamase in complex with 5-diformylaminomethyl-benzo[b]thiophen-2-boronic acid

Template:ABSTRACT PUBMED 17956081

About this Structure

2I72 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy., Venturelli A, Tondi D, Cancian L, Morandi F, Cannazza G, Segatore B, Prati F, Amicosante G, Shoichet BK, Costi MP, J Med Chem. 2007 Nov 15;50(23):5644-54. Epub 2007 Oct 23. PMID:17956081

Page seeded by OCA on Tue Jul 29 04:15:01 2008

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