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Titel:Development of a New Generation of Metal-Based Anticancer Drugs
Autor:Martin, Elisabeth Katharina
Weitere Beteiligte: Meggers, Eric (Prof.Dr.)
URN: urn:nbn:de:hebis:04-z2017-05025
DDC:540 Chemie
Titel (trans.):Entwicklung einer neuen Generation Metall-basierter Krebsmedikamente



Kinases are a large family of transferase enzymes, of which at least 538 different members are present in the human body.[11] By catalysing the transfer of the γ-phosphate group of ATP onto a specific side chain of their substrate, they mediate most cellular signal transductions in the body, thereby regulating various critical cellular activities. These include proliferation, survival, apoptosis, metabolism, transcription, differentiation, and a wide array of other cellular processes.[9,10] It is no surprise that the kinome has been extensively investigated as a family of potential drug targets[12] and the development of kinase inhibitors has therefore become an essential part of biological and medical research. Small molecule kinase inhibitors have been studied to treat various human diseases including cardiovascular diseases,[23] autoimmune disorders such as rheumatoid arthritis,[24] neurodegenerative conditions like Alzheimer’s disease, diabetes or liver disorders.[25] Originally based on unselective natural product inhibitors like staurosporine (51), research has led to almost 30 FDA approved inhibitors by the middle of 2016.[26] Most of them were developed to treat oncological conditions, which are still a major focus of kinase inhibitor research today. Over the last decade the MEGGERS group has established highly potent and selective kinase inhibitors using inert metal centres as unique structural templates, thus mimicking and enhancing the globular shape of the non-selective inhibitor staurosporine (51).

Bibliographie / References

  1. 5. E. K. Martin Development of a new generation of metal-based anticancer drugs. Oral presentation during the 2nd Whole Action Meeting of the COST Action CM1105 at the 1st International Symposium on Functional Metal Complexes that Bind to Biomolecules. (Barcelona, Spain, 09.09.2013 - 10.09.2013).
  2. 3. S. Peukert*, E. Martin, D. Chin, F. Lombardo, E. Meggers. Expanding the druggable chemical space with inert metal-organic complexes. Poster. Gordon Research Conference: Metals in Medicine: Defining the Future of Medicinal Inorganic Chemistry. (Andover, MA, USA, 22.06.2014 - 27.06.2014) * presenting author
  3. 2. E. K. Martin, E. Meggers Development of inert rhodium complexes as potential drug candidates. Poster Presentation. MCB Symposium: Joining forces in pharmaceutical analysis and medicinal chemistry. Awarded the RSC books poster price (Groningen, The Netherlands, 25.08.2014 - 26.08.2014).
  4. 1. E. K. Martin, E. Meggers Drug-like properties of inert metal-based kinase inhibitors. Poster Presentation. Frontiers in Medicinal Chemistry. (Marburg, Germany, 15.03.2015 - 18.03.2015).
  5. 1. R. Rajaratnam, E. K. Martin, M. Dörr, K. Harms, A. Casini, E. Meggers, Nonracemic Octahedral Rhodium-Prolinato Complexes as Protein Kinase Inhibitors, Inorg. Chem., 2015, 54(16), 8111-8120.
  6. 2. E. K. Martin, N. Pagano, M. E. Sherlock, K. Harms, E. Meggers, Synthesis and anticancer activity of ruthenium half-sandwich complexes comprising combined metal centrochirality and planar chirality, Inorg. Chim. Acta, 2014, 423, 530-539.

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