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2blc

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{{STRUCTURE_2blc| PDB=2blc | SCENE= }}
{{STRUCTURE_2blc| PDB=2blc | SCENE= }}
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'''SP21 DOUBLE MUTANT P. VIVAX DIHYDROFOLATE REDUCTASE IN COMPLEX WITH DES-CHLOROPYRIMETHAMINE'''
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===SP21 DOUBLE MUTANT P. VIVAX DIHYDROFOLATE REDUCTASE IN COMPLEX WITH DES-CHLOROPYRIMETHAMINE===
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==Overview==
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Pyrimethamine (Pyr) targets dihydrofolate reductase of Plasmodium vivax (PvDHFR) as well as other malarial parasites, but its use as antimalarial is hampered by the widespread high resistance. Comparison of the crystal structures of PvDHFR from wild-type and the Pyr-resistant (SP21, Ser-58 --&gt; Arg + Ser-117 --&gt; Asn) strain as complexes with NADPH and Pyr or its analog lacking p-Cl (Pyr20) clearly shows that the steric conflict arising from the side chain of Asn-117 in the mutant enzyme, accompanied by the loss of binding to Ser-120, is mainly responsible for the reduction in binding of Pyr. Pyr20 still effectively inhibits both the wild-type and SP21 proteins, and the x-ray structures of these complexes show how Pyr20 fits into both active sites without steric strain. These structural insights suggest a general approach for developing new generations of antimalarial DHFR inhibitors that, by only occupying substrate space of the active site, would retain binding affinity with the mutant enzymes.
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{{ABSTRACT_PUBMED_16135570}}
==About this Structure==
==About this Structure==
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[[Category: Pyrimethamine]]
[[Category: Pyrimethamine]]
[[Category: Thymidylate synthase]]
[[Category: Thymidylate synthase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:27:05 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 19:19:34 2008''

Revision as of 16:19, 27 July 2008

Image:2blc.png

Template:STRUCTURE 2blc

SP21 DOUBLE MUTANT P. VIVAX DIHYDROFOLATE REDUCTASE IN COMPLEX WITH DES-CHLOROPYRIMETHAMINE

Template:ABSTRACT PUBMED 16135570

About this Structure

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

Reference

Crystal structure of dihydrofolate reductase from Plasmodium vivax: pyrimethamine displacement linked with mutation-induced resistance., Kongsaeree P, Khongsuk P, Leartsakulpanich U, Chitnumsub P, Tarnchompoo B, Walkinshaw MD, Yuthavong Y, Proc Natl Acad Sci U S A. 2005 Sep 13;102(37):13046-51. Epub 2005 Aug 31. PMID:16135570

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