Bulgecin A: a novel inhibitor of binuclear metallo-beta-lactamases
文献类型：期刊论文
| 作者 | Simm, Alan M; Loveridge, E Joel; Crosby, John; Avison, Matthew B; Walsh, Timothy R; Bennett, Peter M |
| 刊名 | The Biochemical journal
 |
| 出版日期 | 2005-05-01 |
| 卷号 | 387期号:Pt 3页码:585-90 |
| ISSN号 | 1470-8728 |
| DOI | 10.1042/BJ20041542 |
| 文献子类 | Article |
| 英文摘要 | Bulgecin A, a sulphonated N-acetyl-D-glucosamine unit linked to a 4-hydroxy-5-hydroxymethylproline ring by a beta-glycosidic linkage, is a novel type of inhibitor for binuclear metallo-beta-lactamases. Using steady-state kinetic analysis with nitrocefin as the beta-lactam substrate, bulgecin A competitively inhibited the metallo-beta-lactamase BceII from Bacillus cereus in its two-zinc form, but failed to inhibit when the enzyme was in the single-zinc form. The competitive inhibition was restored by restoring the second zinc ion. The single-zinc metallo-beta-lactamase from Aeromonas veronii bv. sobria, ImiS, was not inhibited by bulgecin A. The tetrameric L1 metallo-beta-lactamase from Stenotrophomonas maltophilia was subject to partial non-competitive inhibition, which is consistent with a kinetic model in which the enzyme bound to inhibitor retains catalytic activity. Docking experiments support the conclusion that bulgecin A co-ordinates to the zinc II site in metallo-beta-lactamases via the terminal sulphonate group on the sugar moiety. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/266634]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Simm, Alan M |
| 作者单位 | Department of Pathology and Microbiology, University of Bristol, University Walk, Bristol BS8 1TD, UK. A.M |
| 推荐引用方式 GB/T 7714 | Simm, Alan M,Loveridge, E Joel,Crosby, John,et al. Bulgecin A: a novel inhibitor of binuclear metallo-beta-lactamases[J]. The Biochemical journal,2005,387(Pt 3):585-90. |
| APA | Simm, Alan M,Loveridge, E Joel,Crosby, John,Avison, Matthew B,Walsh, Timothy R,&Bennett, Peter M.(2005).Bulgecin A: a novel inhibitor of binuclear metallo-beta-lactamases.The Biochemical journal,387(Pt 3),585-90. |
| MLA | Simm, Alan M,et al."Bulgecin A: a novel inhibitor of binuclear metallo-beta-lactamases".The Biochemical journal 387.Pt 3(2005):585-90. |
入库方式： OAI收割
来源：上海药物研究所
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