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. Author manuscript; available in PMC: 2020 Apr 1.
Published in final edited form as: Cancer Discov. 2019 Mar 13;9(4):482–491. doi: 10.1158/2159-8290.CD-18-1175

Figure 1. Adaptive upregulation of compensatory pathways limits the efficacy of PI3K inhibitors.

Figure 1.

Several adaptive feedback mechanisms that limit complete suppression of PIP3 and the cellular response to PI3K inhibitors have been described. These include FOXO-mediated de-repression of RTKs and de-repression of IRS1, leading to partial maintenance of PIP3. In ER+ breast cancer cells, treatment with PI3K inhibitors induces ERα transcriptional activity via the histone methyltransferase KMT2D.