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. 2018 Mar 10;36(8):808-811.
doi: 10.1200/JCO.2017.77.1899. Epub 2018 Jan 30.

Targeting HER2 by Combination Therapies

Ana Ruiz-Saenz  1 , Mark M Moasser  1
Affiliations

Targeting HER2 by Combination Therapies

Ana Ruiz-Saenz et al. J Clin Oncol. .
No abstract available

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Figures

Figure 1
Figure 1
Schematic shows the expression of HER2 on the surface of HER2-amplified cancer cells as seen on HER2 immunohistochemistry (background image) and as imagined by schematic drawings. The participation of HER2 in HER2-HER2 homodimers and in ligand-induced or uninduced HER2-HER3 heterodimers is demonstrated, and the asymmetric mode by which the kinase domains interact is depicted in these dimers. The result of dimerization is phosphorylation of the signaling tails which initiates a series of intracellular signaling cascades. The extracellular binding site for the antibody therapeutics as well as the intracellular site of action of the small molecule inhibitors are shown. The binding of the small molecule inhibitors within the kinase domain inhibits catalytic function and consequently inhibits phosphorylation of the signaling tails as shown. The binding of the antibodies to the extracellular region may have limited effects on dimerization or signaling but has more pronounced effects on mediating engagement of the immune system which is shown here. HER2 receptors are shown in red; HER3 receptors are shown in green.
See this image and copyright information in PMC

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