Protein phosphatase 2 (PP2), also known as PP2A, ... Drug discovery. Drug treatment resulted in decreased cell viability in both cell lines, with IC 50 of 14.3 μM for HCC827 and 12.4 μM for H3255 (Supplemental Figure 2).

PP2 has been identified as a potential biological target to discover drugs to treat Parkinson's disease and Alzheimer's disease, however as of 2014 it was unclear which isoforms would be most beneficial to target, and also whether activation or inhibition would be most therapeutic. We show here that PP2A is inactive … - Mechanism of Action & Protocol. These results indicate that PP2A activation is a viable therapeutic strategy in TKI-sensitive models of LUAD. FTY720 also acts as a potent activator of protein phosphatase 2A (PP2A), a tumor suppressor found inactivated in chronic and blast crisis CML with wild type or imatinib/dasatinib-resistant BCR-ABL1, Ph + B-ALL, Kit D816V AML, Jak2 V617F+ MPDs and other leukemias/lymphomas. “Our results illustrate that small molecules can be used to activate PP2A complexes with extreme selectivity,” Morita remarks. PP2A is a tumor suppressor found inactivated in different types of cancer. A series of small molecule activators of PP2A (SMAPs), was recently derived from tricyclic neurological drugs such as Chlorpromazine and Clomipramine (Kastrinsky et al., 2015). DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

However, tricyclic neuroleptics have direct PP2A-activating properties and our recent study by Sangodkar and colleagues demonstrated that derivatives of these compounds, known as small-molecule activators of PP2A (SMAP), specifically bind to the PP2A A subunit and facilitate PP2A activation, resulting in reduced oncogenic phenotypes both in vitro and in vivo . FTY720 is also a potent protein phosphatase 2A (PP2A)-activating drug (PAD). Given that protein binding for these compounds is approximately 96%, the free drug concentration (which based upon our studies drives the drug activity) is approximately 1–2 μmol/L for a 10-μmol/L drug dose in 10% serum containing medium. FTY720 (Fingolimod, Gilenya) is a sphingosine analog used as an immunosuppressant in multiple sclerosis patients.


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