CANCER AND INFLAMMATION
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. doi:10.1126/scitranslmed.aaq1093.
The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer. Cell 2021 Jun 10;184(12):3143-3162.e32. doi:10.1016/j.cell.2021.04.022. Epub 2021 May 17.
Direct activation of PP2A for the treatment of tyrosine kinase inhibitor-resistant lung adenocarcinoma. JCI Insight 2019 Feb 21;4(4):e125693. doi: 10.1172/jci.insight.125693.
Activation of tumor suppressor protein PP2A inhibits KRAS-driven tumor growth. J Clin Invest. 2017 Jun 1;127(6):2081-2090. doi: 10.1172/JCI89548.Epub 2017 May 15.
Activation of PP2A and Inhibition of mTOR Synergistically Reduce MYC Signaling and Decrease Tumor Growth in Pancreatic Ductal Adenocarcinoma. Cancer Res. 2019 Jan 1;79(1):209-219. doi: 10.1158/0008-5472.CAN-18-0717.Epub 2018 Nov 2.
Unbiased Proteomic Profiling Uncovers a Targetable GNAS/PKA/PP2A Axis in Small Cell Lung Cancer Stem Cells. Cancer Cell. 2020 Jul 13;38(1):129-143.e7. doi: 10.1016/j.ccell.2020.05.003.Epub 2020 Jun 11.
TBK1 and IKKε act like an OFF switch to limit NLRP3 inflammasome pathway activation. Proc Natl Acad Sci U S A. 2021 Sep 21;118(38):e2009309118. doi: 10.1073/pnas.2009309118.
The Effects of Protein Phosphatase 2A Activation with Novel Tricyclic Sulfonamides on Hepatoblastoma. J Pediatr Surg. 2023 Jun;58(6):1145-1154. doi: 10.1016/j.jpedsurg.2023.02.017.Epub 2023 Feb 17.
Small-Molecule Activators of Protein Phosphatase 2A for the Treatment of Castration-Resistant Prostate Cancer. Cancer Res. 2018 Apr 15;78(8):2065-2080. doi: 10.1158/0008-5472.CAN-17-0123.Epub 2018 Jan 22.
Pre-Clinical Study Evaluating Novel Protein Phosphatase 2A Activators as Therapeutics for Neuroblastoma. Cancers (Basel). 2022 Apr 13;14(8):1952. doi: 10.3390/cancers14081952.
Development of actionable targets of multi-kinase inhibitors (AToMI) screening platform to dissect kinase targets of staurosporines in glioblastoma cells. Sci Rep. 2022 Aug 13;12(1):13796. doi: 10.1038/s41598-022-18118-7.
PP2A-based triple-strike therapy overcomes mitochondrial apoptosis resistance in brain cancer cells. Mol Oncol 2023 Sep;17(9):1803-1820.doi: 10.1002/1878-0261.13488.Epub 2023 Jul 26.
Monotherapy efficacy of blood-brain barrier permeable small molecule reactivators of protein phosphatase 2A in glioblastoma. Brain Commun. 2020 Jan 11;2(1):fcaa002.doi: 10.1093/braincomms/fcaa002.eCollection 2020.
Rapid Characterization of Solid Tumors Using Resonant Sensors. ACS Omega. 2022 Sep 2;7(36):32690-32700. doi: 10.1021/acsomega.2c04345.eCollection 2022 Sep 13
Reengineered tricyclic anti-cancer agents. Bioorg Med Chem. 2015 Oct 1;23(19):6528-34.
Targeting the FOXO1/KLF6 axis regulates EGFR signaling and treatment response. J Clin Invest. 2012 Jul;122(7):2637-51. doi: 10.1172/JCI62058.Epub 2012 Jun 1.
PP2A activation overcomes leptomeningeal dissemination in group 3 medulloblastoma. J. Biol. Chem. (2024) 300 (11) 107892
PP2A activation targets MYCN in neuroblastoma. Cell Death and Disease (2026) 17:42
NEURODEGENERATIVE DISEASES
Direct Activation of Protein Phosphatase 2A (PP2A) by Tricyclic Sulfonamides Ameliorates Alzheimer's Disease Pathogenesis in Cell and Animal Models. Neurotherapeutics. 2020 Jul;17(3):1087-1103. doi: 10.1007/s13311-020-00841-6.
Protein phosphatase 2A as a therapeutic target in inflammation and neurodegeneration. Review Pharmacol Ther 2019 Sep:201:181-201. doi: 10.1016/j.pharmthera.2019.05.016.
RESPIRATORY DISEASES
Small-Molecule Activation of Protein Phosphatase 2A Counters Bleomycin-Induced Fibrosis in Mice. ACS Pharmacol Transl Sci. 2023 Oct 17;6(11):1659-1672. doi: 10.1021/acsptsci.3c00117.eCollection 2023 Nov 10.
Protein Phosphatase 2A Reduces Cigarette Smoke-induced Cathepsin S and Loss of Lung Function. Am J Respir Crit Care Med. 2019 Jul 1;200(1):51-62. doi: 10.1164/rccm.201808-1518OC.
Protein Phosphatase 2A as a Therapeutic Target in Pulmonary Diseases. Review. Medicina (Kaunas) 2023 Aug 26;59(9):1552. doi: 10.3390/medicina59091552.
Chronic Cigarette Smoke Exposure Subdues PP2A Activity by Enhancing Expression of the Oncogene CIP2A. Am J Respir Cell Mol Biol 2018 Dec;59(6):695-705. doi: 10.1165/rcmb.2018-0173OC.
Evaluating Novel Protein Phosphatase 2A Activators as Therapeutics for Emphysema. Am J Respir Cell Mol Biol. 2023 Nov;69(5):533-544. doi: 10.1165/rcmb.2023-0105OC.
Relevance of the PP2A Pathway in the Molecular Mechanisms of Chronic Obstructive Pulmonary Disease. Comment Am J Respir Cell Mol Biol. 2019 Nov;61(5):659-660.
PP2A: A Novel Target to Prevent Cathepsin S-mediated Damage in Smoking-induced Chronic Obstructive Pulmonary Disease. Am J Respir Crit Care Med. 2019 Jul 1;200(1):6-8. doi: 10.1164/rccm.201901-0219ED.
PP2A as a New Player in Chronic Obstructive Pulmonary Disease. Am J Respir Cell Mol Biol. 2018 Dec;59(6):659-660. doi: 10.1165/rcmb.2018-0242ED.
Putting a Novel Emphysema Treatment on the SMAP. Am J Respir Cell Mol Biol. 2023 Nov;69(5):491-492. doi: 10.1165/rcmb.2023-0263ED.
BIOPHYSYCAL STUDIES
Direct observation of small molecule activator binding to single PR65 protein. npj Biosensing (2025)2:2
Small Molecule Activators of Protein Phosphatase 2A Exert Global Stabilising Effects on the Scaffold PR65. PREPRINT
PRESENTATIONS
Targeting therapy induced senescence with small molecule Protein Phosphatase 2A (PP2A) activators to prevent glioblastoma relapse after first line treatment. https://www.researchgate.net/publication/403067338_Abstract_B023_Targeting_therapy_induced_senescence_with_small_molecule_Protein_Phosphatase_2A_PP2A_activators_to_prevent_glioblastoma_relapse_after_first_line_treatment
A small molecule activator of the tumor suppressor phosphatase PP2A overcomes leptomeningeal dissemination in Group 3 medulloblastoma. https://www.researchgate.net/publication/403065209_Abstract_B059_A_small_molecule_activator_of_the_tumor_suppressor_phosphatase_PP2A_overcomes_leptomeningeal_dissemination_in_group_3_medulloblastoma