Small molecule inhibitors of receptor tyrosine kinases

Published on June 16, 2009 Reviewed on April 12, 2022   35 min

A selection of talks on Clinical Practice

Please wait while the transcript is being prepared...
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

Quiz available with full talk access. Request Free Trial or Login.

Hide

Small molecule inhibitors of receptor tyrosine kinases

Embed in course/own notes