Protein kinases regulate many aspects of normal cellular activity. Mutations or changes in the expression of protein kinase genes can therefore cause cancer as well as other diseases. Following the approval of imatinib in 2001, considerable progress has been made in the development of potent and specific small-molecule tyrosine kinase inhibitors (TKIs). To overcome resistance, inhibitors may be applied in combination with other kinase inhibitors, or with other therapeutics. To date, more than 70 TKIs have been approved for various diseases, mainly against tumours. The search for novel compounds in cancer treatment is likely to dominate future research in this field. Kinase inhibitors are also being trialled for the treatment of inflammatory and neurodegenerative diseases. In recent years, inhibitors of Bruton tyrosine kinase (BTKi) are undergoing clinical trials in patients with different forms of multiple sclerosis. These small compounds are able to cross the blood-brain barrier and may act directly on the key cells involved in multiple sclerosis pathology, such as microglia. In summary, the discovery of novel TKIs will remain an important research field over the next few decades.
Prof. Dr. Martin Berghoff
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