Leibniz Drug of the Year
Candidalysin is the Leibniz Drug of the Year 2017
In 2017 the commitee awarded four scientists from two Leibniz Insitutes the prize Leibniz Drug of the Year: Dr. Duncan Wilson (HKI), Dr. Selene Mogavero (HKI), Prof. Thomas Gutsmann (FZB) and Prof. Bernhard Hube (HKI) from Leibniz Institute for Natural Product Research and Infection Biology – Hans Knoell Institute Jena (HKI) and Research Center Borstel Leibniz-Center for Medicine and Biosciences (FZB). Their group was involved in the discovery of the novel fungal cytolytic peptide toxin Candidalysin. According to the committee, this work is of high importance for future clinical development of antimycotics.
Clostrubin and tubugis are Leibniz Drugs of the Year 2016
Since 2014, the “Leibniz Drug of the Year” Award is conferred annually for those, within the Leibniz Association, who developed the most prominent bioactive compound. The commission of the Award found this year two contributions as extremely important for the drug development. Therefore, for the Leibniz Drug of the Year 2016 awarded are teams from Hans Knöll Institute Jena (HKI) and Leibniz Institute of Plant Biochemistry (IPB).
Dr. K. Ishida, Dr. S. Pidot and G. Shabuer (HKI) received award for excellent scientific results achieved for the research of the novel natural product clostrubin. They demonstrated that the clostrubin biosynthetic pathway is essential for the anaerobe to enter an oxygen-rich world (for more information see: Science 2015, 350, 670; Angew. Chem. Int. Ed. 2014, 53, 7856). The discovery of clostrubins will have a major impact on various areas of research, including molecular microbiology, natural product research, crop protection, and infection biology.
Prof. Dr. L. A. Wessjohann, Dr. A. Porzel, Dr. O. Pando, S. Stark, R. Kufka and A. Denkert (IPB) were awarded for excellent scientific results achieved in the research area of the bioactive agents tubugis. This group reported on the first synthesis of natural product tubulysin analogues “tubugis” by means of a combination of three different types of isonitrile based multicomponent reactions in a concise and convergent manner (for more information see: J. Am. Chem. Soc. 2011, 133, 7692). The new cytotoxic tubugis show GI50 values in the low picomolar range. The present findings will encourage further investigations on the application or development of new (combinations of) MCRs as a powerful means for the synthesis of complex natural products and related compounds.
A group from the Leibniz Institut für Molekulare Pharmakologie im Forschungsverbund Berlin e.V. (FMP): Margitta Dathe, Heike Nikolenko and Katrin Jordan was awarded with the Leibniz Drug of the Year 2015 for the work on the recombinant human transglutaminase 1 (rhTH1) encapsulated into liposomes. Development of rhTH1 addresses a disease for which there is an acute need for treatment. This disease, autosomal recessive congenital ichthyosis (ARCI), is a genetic disorder that manifests itself in severe, highly visible skin dysfunction starting at newborn age and affecting patients for their entire lifes. rhTH1 is designed as replacement therapy to substitute the enzyme that is not expressed in ARCI patients. Currently, no drug is available for causative treatment of ARCI, and rhTH1 could therefore be the first of its kind. rhTH1 was developed in a highly successful collaboration and proceeded to an advanced stage for which the data suggest significant potential to enter the clinic. The winners elegantly addressed the formulation issue by developing a liposomal carrier system that contains a cationic lipopeptide. In contrast to the free enzyme, this system is able to overcome the cellular barrier and reach the interior of enzyme-deficient keratinocytes. Encapsulated rhTH1 was shown to normalize the ARCI phenotype in a skin-humanized mouse model, thus demonstrating conceptual feasibility of the treatment. The advanced status of this drug candidate is also evident from the fact that it received orphan drug status.
The prize Leibniz Drug of the Year 2014 was awarded to the team from the Leibniz Institute for Natural Product Research and Infection Biology Hans Knöll Institute (HKI) in Jena: Swantje Behnken, Thorger Lincke, Florian Kloss and Keishi Ishida from the group of Christian Hertweck. They developed a new substance class of Closthioamide which was biosyntheticaly induced and isolated from the anaerobic bacterial strain Clostridium cellulolyticum isoliert, as well as chemicaly synthesized. The new compound exhibited antibacterial activity against problematic germs as MRSA.
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