Abstract
The intrinsic qualities of lanthipeptides for their use as therapeutic drugs present several challenges because of their properties, which include stability, solubility and bioavailability, which, under physiological conditions, are very low. Researches have encouraged clinical evaluation of a few compounds, such as mutacin 1140, microbisporicin, actagardine and duramycin, with pharmacokinetic profiles showing rapid distribution and elimination rates, good bioavailability and fecal excretion, as well as high protein binding. Local and parenteral administration are currently suitable to minimize environmental influences on lanthipeptides and ensure efficient activity. Nevertheless, valuable improvements on pharmacodynamic and pharmacokinetic properties may also permit systemic applications via enteral routes. Understanding how rational modifications influence the desired pharmacological and pharmacokinetic properties of these biomolecules would help to answer some specific questions about their susceptibility to environmental changes, mechanism of action and how to engineer other peptides of the same group to improve their clinical relevance.
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Acknowledgements
This work is part of the Cluster of Excellence “Unifying Concepts in Catalysis” coordinated by the Technische Universität Berlin and its graduate school, Berlin International Graduate School of Natural Sciences and Engineering (BIG-NSE). PN and OEL are thankful for the support of this program. OEL obtained a grant from the Graduate School Scholarship Programme of the German Academic Exchange Service (DAAD). Funding was provided by Deutsche Forschungsgemeinschaft (Grant No. EXC 314), Deutscher Akademischer Austauschdienst.
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The original version of this article was revised: corresponding authors name had been corrected.
An erratum to this article is available at http://dx.doi.org/10.1007/s10529-017-2288-3.
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Ongey, E.L., Yassi, H., Pflugmacher, S. et al. Pharmacological and pharmacokinetic properties of lanthipeptides undergoing clinical studies. Biotechnol Lett 39, 473–482 (2017). https://doi.org/10.1007/s10529-016-2279-9
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DOI: https://doi.org/10.1007/s10529-016-2279-9