2o2y

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{{STRUCTURE_2o2y| PDB=2o2y | SCENE= }}
{{STRUCTURE_2o2y| PDB=2o2y | SCENE= }}
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'''The crystal structure of P. falciparum enoyl acyl carrier protein reductase'''
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===The crystal structure of P. falciparum enoyl acyl carrier protein reductase===
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==Overview==
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Recent studies have demonstrated that submicromolar concentrations of the biocide triclosan arrest the growth of the apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii and inhibit the activity of the apicomplexan enoyl acyl carrier protein reductase (ENR). The crystal structures of T. gondii and P. falciparum ENR in complex with NAD(+) and triclosan and of T. gondii ENR in an apo form have been solved to 2.6, 2.2 and 2.8 A, respectively. The structures of T. gondii ENR have revealed that, as in its bacterial and plant homologues, a loop region which flanks the active site becomes ordered upon inhibitor binding, resulting in the slow tight binding of triclosan. In addition, the T. gondii ENR-triclosan complex reveals the folding of a hydrophilic insert common to the apicomplexan family that flanks the substrate-binding domain and is disordered in all other reported apicomplexan ENR structures. Structural comparison of the apicomplexan ENR structures with their bacterial and plant counterparts has revealed that although the active sites of the parasite enzymes are broadly similar to those of their bacterial counterparts, there are a number of important differences within the drug-binding pocket that reduce the packing interactions formed with several inhibitors in the apicomplexan ENR enzymes. Together with other significant structural differences, this provides a possible explanation of the lower affinity of the parasite ENR enzyme family for aminopyridine-based inhibitors, suggesting that an effective antiparasitic agent may well be distinct from equivalent antimicrobials.
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(as it appears on PubMed at http://www.pubmed.gov), where 17327670 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17327670}}
==About this Structure==
==About this Structure==
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==Reference==
==Reference==
Studies of Toxoplasma gondii and Plasmodium falciparum enoyl acyl carrier protein reductase and implications for the development of antiparasitic agents., Muench SP, Prigge ST, McLeod R, Rafferty JB, Kirisits MJ, Roberts CW, Mui EJ, Rice DW, Acta Crystallogr D Biol Crystallogr. 2007 Mar;63(Pt 3):328-38. Epub 2007, Feb 21. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17327670 17327670]
Studies of Toxoplasma gondii and Plasmodium falciparum enoyl acyl carrier protein reductase and implications for the development of antiparasitic agents., Muench SP, Prigge ST, McLeod R, Rafferty JB, Kirisits MJ, Roberts CW, Mui EJ, Rice DW, Acta Crystallogr D Biol Crystallogr. 2007 Mar;63(Pt 3):328-38. Epub 2007, Feb 21. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17327670 17327670]
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Expression, purification and crystallization of the Plasmodium falciparum enoyl reductase., Muench SP, Rafferty JB, McLeod R, Rice DW, Prigge ST, Acta Crystallogr D Biol Crystallogr. 2003 Jul;59(Pt 7):1246-8. Epub 2003, Jun 27. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12832774 12832774]
[[Category: Plasmodium falciparum]]
[[Category: Plasmodium falciparum]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Rossmann fold]]
[[Category: Rossmann fold]]
[[Category: Triclosan binding]]
[[Category: Triclosan binding]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 10:15:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:16:39 2008''

Revision as of 09:16, 28 July 2008

Image:2o2y.png

Template:STRUCTURE 2o2y

The crystal structure of P. falciparum enoyl acyl carrier protein reductase

Template:ABSTRACT PUBMED 17327670

About this Structure

2O2Y is a Single protein structure of sequence from Plasmodium falciparum. Full crystallographic information is available from OCA.

Reference

Studies of Toxoplasma gondii and Plasmodium falciparum enoyl acyl carrier protein reductase and implications for the development of antiparasitic agents., Muench SP, Prigge ST, McLeod R, Rafferty JB, Kirisits MJ, Roberts CW, Mui EJ, Rice DW, Acta Crystallogr D Biol Crystallogr. 2007 Mar;63(Pt 3):328-38. Epub 2007, Feb 21. PMID:17327670

Expression, purification and crystallization of the Plasmodium falciparum enoyl reductase., Muench SP, Rafferty JB, McLeod R, Rice DW, Prigge ST, Acta Crystallogr D Biol Crystallogr. 2003 Jul;59(Pt 7):1246-8. Epub 2003, Jun 27. PMID:12832774

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