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Here you can find the latest news about the activities of the Helmholtz Drug Research.


Significant steps taken in the development of potential new cancer treatments

Chemists in the Drug Discovery Group at the DKFZ, led by Dr. Aubry Miller, in collaboration with scientists from the European Lead Factory (ELF), discovered a novel series of potent and selective inhibitors of the serine protease KLK6

Together with the European Lead Factory (ELF), scientists from the German Cancer Research Center (DKFZ) have successfully discovered potent and selective inhibitors of enzymes associated with the development of some cancers and neurodegenerative diseases. Published in ChemMedChem, the findings mark a significant step in the development of potential new cancer treatments.

The DKFZ scientists collaborated with ELF Partners BioAscent (Scotland) and the Netherlands-based Pivot Park Screening Centre. With their combined expertise in cancer biology, medicinal and synthetic chemistry, DKFZ and the ELF teams developed highly effective chemical leads against Kallikrein-related peptidase 6 (KLK6), the protein that was initially identified as potentially playing a role in the development of some cancers, including colon cancer and melanomas. Subsequent profiling showed that one of the KLK6 compounds reduced the invasion of colon cancer (HCT116) cells in a dose-dependent manner.

These results demonstrate the successful outcomes that can arise from collaboration with the IMI-funded European Lead Factory, and the strengths of providing scientific teams with access to state-of-the-art equipment and screening facilities.

Original Publication:

Dr. Elena De Vita, Niels Smits, Dr. Helma van den Hurk, Dr. Elizabeth M. Beck, Dr. Joanne Hewitt, Dr. Gemma Baillie, Emily Russell, Dr. Andrew Pannifer, Dr. Véronique Hamon, Dr. Angus Morrison, Dr. Stuart P. McElroy, Dr. Philip Jones, Dr. Natalia A. Ignatenko, Dr. Nikolas Gunkel, Dr. Aubry K. Miller. Synthesis and Structure‐Activity Relationships of N‐(4‐Benzamidino)‐Oxazolidinones: Potent and Selective Inhibitors of Kallikrein‐Related Peptidase 6. ChemMedChem 2019 DOI: 10.1002/cmdc.201900536

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