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1ceq

From Proteopedia

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[[Image:1ceq.jpg|left|200px]]
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{{STRUCTURE_1ceq| PDB=1ceq | SCENE= }}
{{STRUCTURE_1ceq| PDB=1ceq | SCENE= }}
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'''CHLOROQUINE BINDS IN THE COFACTOR BINDING SITE OF PLASMODIUM FALCIPARUM LACTATE DEHYDROGENASE.'''
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===CHLOROQUINE BINDS IN THE COFACTOR BINDING SITE OF PLASMODIUM FALCIPARUM LACTATE DEHYDROGENASE.===
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==Overview==
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Although the molecular mechanism by which chloroquine exerts its effects on the malarial parasite Plasmodium falciparum remains unclear, the drug has previously been found to interact specifically with the glycolytic enzyme lactate dehydrogenase from the parasite. In this study we have determined the crystal structure of the complex between chloroquine and P. falciparum lactate dehydrogenase. The bound chloroquine is clearly seen within the NADH binding pocket of the enzyme, occupying a position similar to that of the adenyl ring of the cofactor. Chloroquine hence competes with NADH for binding to the enzyme, acting as a competitive inhibitor for this critical glycolytic enzyme. Specific interactions between the drug and amino acids unique to the malarial form of the enzyme suggest this binding is selective. Inhibition studies confirm that chloroquine acts as a weak inhibitor of lactate dehydrogenase, with mild selectivity for the parasite enzyme. As chloroquine has been shown to accumulate to millimolar concentrations within the food vacuole in the gut of the parasite, even low levels of inhibition may contribute to the biological efficacy of the drug. The structure of this enzyme-inhibitor complex provides a template from which the quinoline moiety might be modified to develop more efficient inhibitors of the enzyme.
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The line below this paragraph, {{ABSTRACT_PUBMED_10187806}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 10187806 is the PubMed ID number.
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{{ABSTRACT_PUBMED_10187806}}
==About this Structure==
==About this Structure==
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[[Category: Oxidoreductase]]
[[Category: Oxidoreductase]]
[[Category: Tricarboxylic acid cycle]]
[[Category: Tricarboxylic acid cycle]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 12:39:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jun 30 20:38:46 2008''

Revision as of 17:38, 30 June 2008

Image:1ceq.png

Template:STRUCTURE 1ceq

CHLOROQUINE BINDS IN THE COFACTOR BINDING SITE OF PLASMODIUM FALCIPARUM LACTATE DEHYDROGENASE.

Template:ABSTRACT PUBMED 10187806

About this Structure

1CEQ is a Single protein structure of sequence from Plasmodium falciparum. Full crystallographic information is available from OCA.

Reference

Chloroquine binds in the cofactor binding site of Plasmodium falciparum lactate dehydrogenase., Read JA, Wilkinson KW, Tranter R, Sessions RB, Brady RL, J Biol Chem. 1999 Apr 9;274(15):10213-8. PMID:10187806

Page seeded by OCA on Mon Jun 30 20:38:46 2008

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