Figure 3. Strategies for multi-targeted kinase inhibition.
a | The single agent PP121 was shown to target both tyrosine kinases (such as vascular endothelial growth factor receptor 2, BCR–ABL and RET) and PI3K family members such as PIK3CA and mTOR (inhibitor targets are shown in red boxes). Note that the combined inhibition of mTOR and PI3K by PP121 disables a negative feedback loop in which mTOR inhibits PI3K. b | the combination of the MEK inhibitor AZD6244 and the Akt inhibitor MK-2206 results in the inhibition of both the MAPK and PI3K pathways. This combination is being evaluated in clinical trials. RTK, receptor tyrosine kinase.