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Printable Handouts
Navigable Slide Index
- Introduction
- Protein tyrosine kinases (TKs)
- Phosphorylation of tyrosine residues
- Two classes of TKs
- Nonreceptor TKs
- Receptor TKs (1)
- Receptor and nonreceptor TKs
- Receptor TKs (2)
- Activation of receptor TKs
- The effects of rTK activation
- Mechanisms of TK dysregulation in cancer
- Consequences of TK activation in cancer
- Strategies to target TKs in cancer therapy
- CML- a model disease for science advancement
- Chronic myeloid leukaemia (CML)
- 1960 - discovery of the Philadelphia chromosome
- 1973 - the first description of human oncogene
- 1990- BCR-ABL causes CML in mice
- Imatinib specifically targets BCR-ABL oncogene
- Imatinib mesylate (1)
- Imatinib mesylate (2)
- Imatinib- the IRIS trial
- Targeting other rTKs
- rTK dysregulation in cancer
- Mutations in rTKs lead to constitutive activation
- Epidermal growth factor receptor (EGFR)
- Small molecule inhibitors of EGFR
- Factors predicting response to EGFR TK inhibitors
- Cetuximab
- Her-2/neu
- Herceptin
- C-KIT
- PDGFR
- Sites of KIT and PDGFR alpha mutations in GIST
- Treatment paradigms for the treatment of GIST
- Imatinib targets in solid tumours
- FLT3: a major target in AML
- Direct inhibitors of FLT3
- C-MET
- Small-molecule MET inhibitors
- Vascular endothelial growth factor (receptor)
- Completed anti-VEGF therapy phase III trials
- Bevacizumab
- Fibroblast growth factor receptor 3 (FGFR 3)
- Other TK targets in hematologic malignancies
- Simultaneous inhibition of two TKs
- Vandetanib (ZD6474) and AZD2171
- Multitargeted TKIs: sunitinib malate
- Biological effects of sunitinib
- Properties of sunitinib malate
- Multitargeted TKIs: sorafenib
- Limitations of TK therapy: toxicity
- The unexpected cardiotoxicity of imatinib
- Limitations of TK therapy: resistance
- Limitations of TK therapy: resistance to mAbs
- Problems with imatinib
- Mechanisms of resistance to TKI therapy
- The development of resistance to imatinib
- Imatinib-resistant mutations in BCR-ABL
- Resistance mechanism
- T315I - "the mutation from hell"
- BMS-354825 (dasatinib)
- Imatinib resistant CML cells
- Overcoming resistance
- Identifying new targets
- The drug development process for TKIs
- Targeted therapy in haematological malignancies
- Targeted therapy in solid tumours
- Summary
Topics Covered
- Overview of tyrosine kinases
- Tyrosine kinase dysregulation in cancer
- The example of chronic myelogenous leukemia
- Receptor tyrosine kinases: function and involvement in cancer, treatment with small molecule inhibitors to these tyrosine kinases
- Inhibition of several tyrosine kinases
- Toxicity
- Resistance
- The future of treatment with tyrosine kinase inhibitors
Links
Series:
Categories:
Therapeutic Areas:
Talk Citation
Krause, D. (2009, June 16). Small molecule inhibitors of receptor tyrosine kinases [Video file]. In The Biomedical & Life Sciences Collection, Henry Stewart Talks. Retrieved December 14, 2019, from https://hstalks.com/bs/1321/.Publication History
Financial Disclosures
- Dr. Daniela Krause has not informed HSTalks of any commercial/financial relationship that it is appropriate to disclose.
Small molecule inhibitors of receptor tyrosine kinases
Published on June 16, 2009
35 min