Development of a New Generation of Metal-Based Anticancer Drugs
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, ther...
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| Format: | Dissertation |
| Sprache: | Englisch |
| Veröffentlicht: |
Philipps-Universität Marburg
2017
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| Online-Zugang: | PDF-Volltext |
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| Zusammenfassung: | 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). |
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| Umfang: | 315 Seiten |
| DOI: | 10.17192/z2017.0502 |