Malarial Dihydrofolate Reductase as Drug Target
From Proteopedia
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<StructureSection load='3QGT' size='350' side='right' caption='Crystal structure of Wild-type PfDHFR-TS COMPLEXED WITH NADPH, dUMP AND PYRIMETHAMINE (PDB entry [[3QGT]])' scene=''> | <StructureSection load='3QGT' size='350' side='right' caption='Crystal structure of Wild-type PfDHFR-TS COMPLEXED WITH NADPH, dUMP AND PYRIMETHAMINE (PDB entry [[3QGT]])' scene=''> | ||
| - | + | Mutant, Drug Resistant PfDHFR | |
---- | ---- | ||
The | The | ||
| - | <scene name='Malarial_Dihydrofolate_Reductase_as_Drug_Target/Quadruple_mutant/1'>quadruple mutant</scene> of PfDHFR has four <scene name='Malarial_Dihydrofolate_Reductase_as_Drug_Target/Mutated_codons/1'>point mutations</scene> | + | <scene name='Malarial_Dihydrofolate_Reductase_as_Drug_Target/Quadruple_mutant/1'>quadruple mutant</scene> of PfDHFR has four <scene name='Malarial_Dihydrofolate_Reductase_as_Drug_Target/Mutated_codons/1'>point mutations</scene>: |
| - | </StructureSection> | + | </StructureSection> N51I, C59R, S108N, and I164L. These mutations caused decreased binding affinities of inhibitors similar to pyrimethamine. |
Revision as of 05:47, 28 November 2012
Introduction
There are currently antimalarial drugs that target the malarial dihydrofolate reductase (DHFR) such as pyrimethamine and cycloguanil. However, the effectiveness of these drugs has decreased because of mutations in the enzyme that have led to drug resistance. New research in drug development now incorporates both the wild-type as well as the quadruple mutant DHFR from the Plasmodium falciparum malarial strain.
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Proteopedia Page Contributors and Editors (what is this?)
Mary Smith, Alexander Berchansky, Karsten Theis, Michal Harel
