Small molecule inhibitors of receptor tyrosine kinases

Published on June 16, 2009 Reviewed on December 4, 2019   35 min

Other Talks in the Therapeutic Area: Oncology

0:00
My name is Daniela Krause from Massachusetts General Hospital in Boston, and I'm going to talk about small molecule inhibitors of receptor tyrosine kinases. Since the arrival of imatinib up for the treatment of chronic myelogenous leukemia in 2001 the use of other small molecule inhibitors of tyrosine kinases has experienced increasing popularity over the last few years. This really is the great story of the successful translation of findings from basic research to clinical medicine, but also poses the question about the future of modern medicine.
0:34
Tyrosine kinases belong to large group of protein kinases they're enzymes that can transfer a phosphate group from ATP to a tyrosine residue in a protein. The human genome contains 90 tyrosine kinases and 43 tyrosine kinase like genes, they regulate cellular proliferation, survival, differentiation, function and motility. They have largely been ignored for the last 25 years in drug development because of paucity of evidence for a causative role in human cancer and concerns about drug specificity and toxicity. But since the arrival of imatinib, it was realized that tyrosine kinase inhibitors can be used in specific cancers in which a mutation that causes certain tyrosine kinasaes to be constitutively active.
1:21
Tyrosine kinases catalyze the transfer of phosphate, as you can see on the top left from ATP onto tyrosine residues, as you can see on the top right onto proteins.
1:33
Two classes of tyrosine kinases exist. Receptor tyrosine kinases and non-receptor tyrosine kinases. Nonreceptor tyrosine kinases lack transmembrane domains, and
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Small molecule inhibitors of receptor tyrosine kinases

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