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Reliable, easy-to-read patient information on common medical conditions β€” written in plain language, free of jargon, and grounded in current evidence. Browse the most frequent diagnoses, understand what they mean for everyday life, and learn which steps and questions help you have a focused conversation with your doctor.

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Platensimycin

Introduction

Platensimycin is a member of a previously unknown class of antibiotics, which acts by blocking enzymes involved in the of the condensation steps in fatty acid biosynthesis,[1] which bacteria need to biosynthesise cell membranes (Ξ²-ketoacyl-(acyl-carrier-protein (ACP)) synthase I/II (FabF/FabB). Other enzymes in this pathway have similarly been proven antibiotic targets for example FabI, the enoyl-ACP (acyl carrier protein) reductase, that is inhibited by isoniazid and related compounds and the antiseptic agent triclosan.[2] It is an experimental new drug in preclinical trials in an effort to combat MRSA in a mouse model.[3] The newly discovered natural product inhibitor was first isolated from a strain of Streptomyces platensis by the Merck group.[3]

Recently, a first total synthesis of racemic platensimycin has been published.[4] Its structure consists of a 3-amino-2,4-dihydroxybenzoic acid polar part linked through an amine bond to a lipophilic pentacyclicketolide.[4]

References

  1. ↑ Dieter HΓ€bich, Franz von Nussbaum, ChemMedChem 2006, 1, 951–954. Platensimycin, a new antibiotic and “superbug challenger” from nature. PMID 16952137
  2. ↑ H T. Wright, and K.A Reynolds (2007) Antibacterial targets in fatty acid biosynthesis. Current Opinion in Microbiology doi:10.1016/j.mib.2007.07.001
  3. ↑ 3.0 3.1 Jun Wang et al, Platensimycin is a selective FabF inhibitor with potent antibiotic properties, Nature 441, 358-361 (18 May 2006) PMID 16710421
  4. ↑ 4.0 4.1 K. C. Nicolaou, A. Li, D. J. Edmonds, Angew. Chem. 2006, 118, 7244 – 7248; Angew. Chem. Int. Ed. 2006, 45, 7086 – 7090. PMID 17013803

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