Platensimycin

Structural formula
General
Surname	Platensimycin
Molecular formula	C 24 H 27 NO 7
External identifiers / databases
CAS number 835876-32-9 PubChem 6857724 ChemSpider 5257055 DrugBank DB08407 Wikidata Q423275
Drug information
Drug class	antibiotic
properties
Molar mass	441.47 g mol −1
safety instructions
GHS hazard labeling no classification available
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Platensimycin is a newly discovered antibiotic . This substance is the first representative of a previously unknown structural class of antibiotics . Researchers from MSD Sharp & Dohme found platensimycin as part of a substance screening project. It is produced by the bacterium Streptomyces platensis , which was found in a South African soil sample. A first total chemical synthesis of racemic platensimycin was described in 2006.

Mechanism of action

Platensimycin inhibits a key enzyme called FabF and thus selectively inhibits a bacterial synthetase that bacteria need to build up the fatty acid on the surface and cell membrane. Few known antibiotics inhibit bacterial fatty acid - Synthesis . Because it has a different mechanism of action than conventional antibiotics, it is assumed that far fewer bacteria become resistant to platensimycin.

Study situation

Platensimycin was shown to be effective in mice against multi - resistant gram-positive germs such as MRSA , for which vancomycin is the last reserve antibiotic to date . Platensimycin was found to be a very effective antibiotic when continuously administered to cells in vivo, but its effectiveness was reduced when other common routes of administration were used. Another disadvantage is the high doses required for effectiveness in animal experiments. That is why attempts to change the structure in favor of greater effectiveness are preferred to clinical studies.

Individual evidence

1. ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
2. ↑ Jun Wang et al., Platensimycin is a selective FabF inhibitor with potent antibiotic properties . In; Nature . 2006, 441, pp. 358-361, PMID 16710421 .
3. ↑ KC Nicolaou , A. Li, DJ Edmonds, Angew. Chem. 2006 , 118 , 7244-7248; Angew. Chem. Int. Ed. 2006 , 45 , 7086-7090, PMID 17013803 .
4. ^ Heath RJ, White SW, Rock CO: Inhibitors of fatty acid synthesis as antimicrobial chemotherapeutics. In: Appl Microbiol Biotechnol. 2002, 58.6, pp. 695-703. Epub 2002 Mar 7, PMID 12021787 .
5. ↑ Dieter Häbich, Franz von Nussbaum: Platensimycin, a new antibiotic and "superbug challenger" from nature. In: ChemMedChem . 2006, 1, pp. 951-954. PMID 16952137 .
6. ↑ Potent antibiotic to target MRSA . In: BBC News . May 18, 2006. Retrieved December 14, 2009.
7. ↑ K B. Herath, A B. Attygalle, and S B. Singh: Biosynthetic Studies of Platensimycin . In: J. Am. Chem. Soc. 2007, 129, 50, pp. 15422-15423, PMID 18034483 .
8. ↑ Michael J. Smanski, Ryan M. Peterson, Scott R. Rajski, Ben Shen: Engineered Streptomyces platensis Strains That Overproduce Antibiotics Platensimycin and Platencin. In: Antimicrobial Agents and Chemotherapy . 2009, 53,4, pp. 1299-1304, doi : 10.1128 / AAC.01358-08 .

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