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3FRB

S. aureus F98Y DHFR complexed with TMP

Summary for 3FRB
Entry DOI10.2210/pdb3frb/pdb
Related3FRA 3FRD 3FRE 3FRF
DescriptorDihydrofolate reductase, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, TRIMETHOPRIM, ... (4 entities in total)
Functional Keywordss. aureus dhfr, oxidoreductase, nadp, one-carbon metabolism
Biological sourceStaphylococcus aureus
Total number of polymer chains1
Total formula weight19194.46
Authors
Oefner, C.,Dale-Glenn, E. (deposition date: 2009-01-08, release date: 2010-01-12, Last modification date: 2024-05-29)
Primary citationOefner, C.,Bandera, M.,Haldimann, A.,Laue, H.,Schulz, H.,Mukhija, S.,Parisi, S.,Weiss, L.,Lociuro, S.,Dale, G.E.
Increased hydrophobic interactions of iclaprim with Staphylococcus aureus dihydrofolate reductase are responsible for the increase in affinity and antibacterial activity
J.Antimicrob.Chemother., 63:687-698, 2009
Cited by
PubMed Abstract: Iclaprim is a novel 2,4-diaminopyrimidine that exhibits potent, rapid bactericidal activity against major Gram-positive pathogens, including methicillin-susceptible Staphylococcus aureus and methicillin-resistant S. aureus, and is currently in clinical development for the treatment of complicated skin and skin structure infections. An understanding of the known mechanism of resistance to trimethoprim led to the design of this new inhibitor, with improved affinity towards dihydrofolate reductase (DHFR) from S. aureus and clinically useful activity against S. aureus including isolates resistant to trimethoprim. The objective of this study was to characterize the mode of action of iclaprim and its inhibitory properties against DHFR.
PubMed: 19211577
DOI: 10.1093/jac/dkp024
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2 Å)
Structure validation

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