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Review
. 2009 Aug 27;52(16):4981-5004.
doi: 10.1021/jm9002395.

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach

Rongshi Li  1 , Alan Pourpak, Stephan W Morris
Affiliations
Review

Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach

Rongshi Li et al. J Med Chem. .
No abstract available

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Figures

Figure 1
Figure 1
The major signaling pathways activated by the IGF1R. The RAS/RAF/MEK/ERK and PI3K/AKT pathways are depicted above. The IGF1R is activated by binding of either IGF1 or IGF2. Binding of ligand induces a conformational change and autophosphorylation of key residues in the β subunits of the receptor, and docking proteins then interact with the phosphorylated residues of the activated receptor. Activation of the receptor and transduction of the intracellular signaling kinase cascades culminates in cell proliferation and anti-apoptotic effects. Detailed descriptions of the regulation of IGF1R activation and of these signaling pathways can be found in Sections 2a and b.
Figure 2
Figure 2
Structures of kinase inhibitors approved for cancer therapy.
Figure 3
Figure 3
Structures of ATP-competitive inhibitors (I).
Figure 4
Figure 4
Structures of ATP-competitive inhibitors (II).
Figure 5
Figure 5
Structures of ATP-competitive inhibitors (III).
Figure 6
Figure 6
Structures of ATP-noncompetitive or “mechanism unknown” inhibitors.
See this image and copyright information in PMC

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