Akt (protein kinase B) is a key regulator in a variety of cellular processes such as glucose metabolism, cell survival, proliferation and cell migration. Its activity is aberrantly upregulated in a plethora of cancers, metabolic and immune disorders, including but not limited to breast, pancreatic and prostate cancer. More specific, time-resolved monitoring of key drivers of metabolism and proliferation in tissue specific contexts can be achieved in an in vivo setting with the use of FRET-biosensor mice to track protein activity and the effect of therapeutic intervention.
Here, we describe the generation and characterization of a FRET-biosensor mouse to examine Akt [1.] activity in an in vivo setting in a variety of tissues and cancers by the application of optical windows [2.]. Elevated levels of Akt activity were observed in the pancreatic cancer models driven by mutant KRasG12D/+ and KRasG12D/+;p53R172H/+, including PTEN loss driven PDAC as reported previously [3.] and Akt activity mapped over the course of disease progression. Whole body PTENG129E/+ mutation or loss (PTENfloxed/+) mice were also crossed to the Akt-FRET biosensor mouse and Akt activity measured in several cancers such as lymphomas, adrenal, mammary and prostate cancer. Cell lines and organoid cultures established from these tumours retained the AKT-FRET reporter expression and inhibition of Akt was mapped in vitro over time in 2D and 3D contexts. Akt activity was also effectively inhibited by administration of a Pi3K inhibitor and pharmacodynamics mapped live in vivo in a breast cancer setting. Akt activity was further successfully quantified in a variety of tissues by specific Cre driver lines such as in the brain via neuropeptide Y receptor-Cre (NPY-Cre), in pancreatic beta islets (RIP-Cre) or in the entire pancreas (Pdx1-Cre). Metabolic challenge in mice bearing optical windows over the pancreas (RIP-Cre), white fat or brown fat was moreover successfully imaged live in vivo in Akt-FRET mice following ip administration of glucose or insulin.
In conclusion, the described Akt-FRET biosensor mouse can be applied to a wide range of metabolic, immune and cancer settings and used successfully in characterizing disease etiology and monitoring treatment outcomes.