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脂肪酸合成抑制剂平板霉素的开发

Fatty acid synthesis inhibitor:platensimycin
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摘要 平板霉素为平板链球菌(Streptomyces platensis)的代谢产物,其独特的化学结构和良好的抗菌活性引人关注。平板素及其他系列同类物的开发,改善了平板霉素的体内药动学不稳定性。本文综述平板霉素的抗菌原理与活性、同类物开发和基因改造。 Platensimycin is the metabolite of Streptomyces platensis. Because of its novel chemical structure and antibacterial activity, more and more attention has been paid on it. The development of platencin and its analogs can improve the stability of platensimycin. This review summarizes antibacterial activities and mechanism of platensimycin, as well as development of its analogs and genetic modification.
作者 王林婧 胡海峰
机构地区 上海医药工业研究院创新药物与制药工艺国家重点实验室
出处 《世界临床药物》 CAS 2011年第12期738-741,共4页 World Clinical Drug
基金 微生物药物技术创新与新药创制产学研联盟(2010ZX09401-403)
关键词 脂肪酸合成抑制剂 平板霉素 平板素 抗生素 生物合成 药物开发 Fatty acid synthesis inhibitors platensimycin platencin antibiotics biosynthesis drug development
分类号 R978.1 [医药卫生—药品]
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  • 1Wang J, Soisson. SM, Young K, et al. Platensimycin is a selective FabF inhibitor with potent antibiotic properties [J].Nature, 2006, 441 (7091) : 358-361.
  • 2Young K, Jayasuriya H, Ondeyka JG, et al. Discovery of FabH/FabF inhibitors from natural products [J]. Antimicrob Agents Ch, 2006, 50 (2): 519-526.
  • 3Castillo YP, Perez MAC. Bacterial beta-ketoacyl-acyl carrier protein synthase III (FabH) : an attractive target for the design of new broad-spectrum antimicrobial agents [J]. Mini-Rev Med Chem, 2008, 8 (1) : 36-45.
  • 4Jayasuriya H, Herath KB, Zhang C, et al. Isolation and structure of platencin: a FabH and FabF dual inhibitor with potent broad-spectrum antibiotic activity [J]. Angew Chem Int Edit, 2007, 46 (25) : 4684-4688.
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  • 7Brinster S, Lamberet G, Staels B, et al. Type II fatty acidsynthesis is not a suitable antibiotic target for Gram- positive pathogens [J]. Nature, 2009, 458 (7234) :83-88.
  • 8Wang J, Kodali S, Lee SH, et al. Discovery of platencin, a dual FabF and FabH inhibitor with in vivo antibiotic properties[J]. P Natl Acad Sci USA, 2007, 104(18): 7612-7616.
  • 9Zhang CW, Ondeyka J, Zink DL, et al. Isolation, structure and fatty acid synthesis inhibitory activities of platensimycin B l-B3 from Streptomyces platensis [J]. Chem Commun, 2008, 44 (40) : 5034-5036.
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世界临床药物
2011年 第12期

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