8RM3 の概要
| エントリーDOI | 10.2210/pdb8rm3/pdb |
| 分子名称 | Ferrioxamine receptor FoxA, octyl beta-D-glucopyranoside, GLYCEROL, ... (10 entities in total) |
| 機能のキーワード | tonb-dependent transporter siderophore, membrane protein |
| 由来する生物種 | Pseudomonas aeruginosa PAO1 |
| タンパク質・核酸の鎖数 | 1 |
| 化学式量合計 | 93675.48 |
| 構造登録者 | |
| 主引用文献 | Faucon, A.,Renault, J.,Josts, I.,Couchot, J.,Renaud, J.L.,Hoegy, F.,Plesiat, P.,Tidow, H.,Gaillard, S.,Mislin, G.L.A. Synthesis and antibacterial properties under blue LED light of conjugates between the siderophore desferrioxamine B (DFOB) and an Iridium(III) complex. Bioorg.Med.Chem., 112:117842-117842, 2024 Cited by PubMed Abstract: The decline of antibiotics efficacy worldwide has recently reached a critical point urging for the development of new strategies to regain upper hand on multidrug resistant bacterial strains. In this context, the raise of photodynamic therapy (PDT), initially based on organic photosensitizers (PS) and more recently on organometallic PS, offers promising perspectives. Many PS exert their biological effects through the generation of reactive oxygen species (ROS) able to freely diffuse into and to kill surrounding bacteria. Hijacking of the bacterial iron-uptake systems with siderophore-PS conjugates would specifically target pathogens. Here, we report the synthesis of unprecedented conjugates between the siderophore desferrioxamine B (DFOB) and an antibacterial iridium(III) PS. Redox properties of the new conjugates have been determined at excited states and compared to that of an antibacterial iridium PS previously reported by our groups. Tested on nosocomial pathogen Pseudomonas aeruginosa and other bacteria, these conjugates demonstrated significant inhibitory activity when activated with blue LED light. Ir(III) conjugate and iridium free DFOB-2,2'-dipyridylamine ligands were crystallized in complex with FoxA, the outer membrane transporter involved in DFOB uptake in P. aeruginosa and revealed details of the binding mode of these unprecedented conjugates. PubMed: 39173538DOI: 10.1016/j.bmc.2024.117842 主引用文献が同じPDBエントリー |
| 実験手法 | X-RAY DIFFRACTION (2.22 Å) |
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