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Tyrosine Kinase Inhibitor
No.169(April 2016)
Tyrphostins are a series of the small molecules which are designed to bind to the subsite of the protein tyrosine kinase (PTK) domain.1) Tyrphostin AG494 (1) inhibits tyrosine kinases shown in the table.2-4) 1 also blocks cyclin-dependent kinase 2 (cdk2) activation.5)
References
- 1)Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors
- 2)Tyrphostins. 2. Heterocyclic and α-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinase
- 3)Selective inhibition of the epidermal growth factor and HER2/Neu receptors by tyrphostins
- 4)Tyrosine kinase inhibition: An approach to drug devepolment
- 5)Tyrphostin AG494 blocks Cdk2 activation
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