1vyq

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{{STRUCTURE_1vyq| PDB=1vyq | SCENE= }}
{{STRUCTURE_1vyq| PDB=1vyq | SCENE= }}
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'''NOVEL INHIBITORS OF PLASMODIUM FALCIPARUM DUTPASE PROVIDE A PLATFORM FOR ANTI-MALARIAL DRUG DESIGN'''
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===NOVEL INHIBITORS OF PLASMODIUM FALCIPARUM DUTPASE PROVIDE A PLATFORM FOR ANTI-MALARIAL DRUG DESIGN===
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==Overview==
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Pyrimidine metabolism is a major route for therapeutic intervention against malaria. Here we report inhibition and structural studies on the deoxyuridine nucleotidohydrolase from the malaria parasite Plasmodium falciparum (PfdUTPase). We have identified a series of triphenylmethane derivatives of deoxyuridine with antimalarial activity in vitro which inhibit specifically the Plasmodium dUTPase versus the human enzyme. A 2.4 Angstrom crystal structure of PfdUTPase in complex with one of these inhibitors reveals an atypical trimeric enzyme in which the triphenylmethane derivative can be seen to select for PfdUTPase by way of interactions between the trityl group and the side chains of residues Phe46 and Ile117. Immunofluorescence microscopy studies of parasitized red blood cells reveal that enzyme concentrations are highest during the trophozoite/schizont stages, suggesting that PfdUTPase has a major role in DNA replication. Taken together the data show that PfdUTPase may be considered as an antimalarial drug target.
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(as it appears on PubMed at http://www.pubmed.gov), where 15698576 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15698576}}
==About this Structure==
==About this Structure==
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[[Category: Malaria]]
[[Category: Malaria]]
[[Category: Plasmodium falciparum]]
[[Category: Plasmodium falciparum]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:55:28 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 17:32:57 2008''

Revision as of 14:33, 27 July 2008

Image:1vyq.png

Template:STRUCTURE 1vyq

NOVEL INHIBITORS OF PLASMODIUM FALCIPARUM DUTPASE PROVIDE A PLATFORM FOR ANTI-MALARIAL DRUG DESIGN

Template:ABSTRACT PUBMED 15698576

About this Structure

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

Reference

dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors., Whittingham JL, Leal I, Nguyen C, Kasinathan G, Bell E, Jones AF, Berry C, Benito A, Turkenburg JP, Dodson EJ, Ruiz Perez LM, Wilkinson AJ, Johansson NG, Brun R, Gilbert IH, Gonzalez Pacanowska D, Wilson KS, Structure. 2005 Feb;13(2):329-38. PMID:15698576

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