1mfp

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[[Image:1mfp.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_1mfp| PDB=1mfp | SCENE= }}
{{STRUCTURE_1mfp| PDB=1mfp | SCENE= }}
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'''E. coli Enoyl Reductase in complex with NAD and SB611113'''
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===E. coli Enoyl Reductase in complex with NAD and SB611113===
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==Overview==
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Bacterial enoyl-ACP reductase (FabI) is responsible for catalyzing the final step of bacterial fatty acid biosynthesis and is an attractive target for the development of novel antibacterial agents. Previously we reported the development of FabI inhibitor 4 with narrow spectrum antimicrobial activity and in vivo efficacy against Staphylococcus aureus via intraperitoneal (ip) administration. Through iterative medicinal chemistry aided by X-ray crystal structure analysis, a new series of inhibitors has been developed with greatly increased potency against FabI-containing organisms. Several of these new inhibitors have potent antibacterial activity against multidrug resistant strains of S. aureus, and compound 30 demonstrates exceptional oral (po) in vivo efficacy in a S. aureus infection model in rats. While optimizing FabI inhibitory activity, compounds 29 and 30 were identified as having low micromolar FabK inhibitory activity, thereby increasing the antimicrobial spectrum of these compounds to include the FabK-containing pathogens Streptococcus pneumoniae and Enterococcus faecalis. The results described herein support the hypothesis that bacterial enoyl-ACP reductases are valid targets for antibacterial agents.
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(as it appears on PubMed at http://www.pubmed.gov), where 12699381 is the PubMed ID number.
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{{ABSTRACT_PUBMED_12699381}}
==About this Structure==
==About this Structure==
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[[Category: Enoyl-acp reductase]]
[[Category: Enoyl-acp reductase]]
[[Category: Fabi]]
[[Category: Fabi]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 00:58:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 23:52:08 2008''

Revision as of 20:52, 2 July 2008

Image:1mfp.png

Template:STRUCTURE 1mfp

E. coli Enoyl Reductase in complex with NAD and SB611113

Template:ABSTRACT PUBMED 12699381

About this Structure

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

Reference

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK., Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF, J Med Chem. 2003 Apr 24;46(9):1627-35. PMID:12699381

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