3FRB

S. aureus F98Y DHFR complexed with TMP

3FRB の概要

• エントリーDOI: 10.2210/pdb3frb/pdb
• 関連するPDBエントリー: 3FRA 3FRD 3FRE 3FRF
• 分子名称: Dihydrofolate reductase, NADP NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE, TRIMETHOPRIM, ... (4 entities in total)
• 機能のキーワード: s. aureus dhfr, oxidoreductase, nadp, one-carbon metabolism
• 由来する生物種: Staphylococcus aureus
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 19194.46

構造登録者

Oefner, C.,Dale-Glenn, E. (登録日: 2009-01-08, 公開日: 2010-01-12, 最終更新日: 2024-05-29)

主引用文献

Oefner, 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

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

実験手法

X-RAY DIFFRACTION (2 Å)