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LB100, a small molecule inhibitor of PP2A with potent chemo- and radio-sensitizing potential
Christopher S Hong1, Winson Ho, Chao Zhang
1a The Ohio State University Wexner Medical Center ; Department of Neurological Surgery ; Columbus , OH USA.
Abstract:
Protein phosphatase 2A (PP2A) is a serine/threonine phosphatase that plays a significant role in mitotic progression and cellular responses to DNA damage. While traditionally viewed as a tumor suppressor, inhibition of PP2A has recently come to attention as a novel therapeutic means of driving senescent cancer cells into mitosis and promoting cell death via mitotic catastrophe. These findings have been corroborated in numerous studies utilizing naturally produced compounds that selectively inhibit PP2A. To overcome the known human toxicities associated with these compounds, a water-soluble small molecule inhibitor, LB100, was recently developed to competitively inhibit the PP2A protein. This review summarizes the pre-clinical studies to date that have demonstrated the anti-cancer activity of LB100 via its chemo- and radio-sensitizing properties. These studies demonstrate the tremendous therapeutic potential of LB100 in a variety of cancer types. The results of an ongoing phase 1 trial are eagerly anticipated.
Insights
Protein phosphatase 2A (PP2A) inhibition shows promise for cancer therapy. The novel inhibitor LB100 sensitizes tumors to chemotherapy and radiation, potentially leading to cancer cell death.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Protein phosphatase 2A (PP2A) is crucial for cell division and DNA damage response.
- PP2A traditionally acts as a tumor suppressor.
- Inhibiting PP2A can induce senescent cancer cells to undergo mitosis and cell death.
Purpose of the Study:
- To review preclinical studies on the anti-cancer activity of LB100.
- To highlight LB100's chemo- and radio-sensitizing properties.
- To assess the therapeutic potential of LB100 in various cancers.
Main Methods:
- Review of preclinical research on LB100.
- Analysis of LB100's mechanism as a PP2A inhibitor.
- Evaluation of LB100's efficacy in sensitizing cancer cells.
Main Results:
- LB100, a water-soluble PP2A inhibitor, overcomes toxicities of natural compounds.
- Preclinical studies demonstrate LB100's anti-cancer effects.
- LB100 exhibits significant chemo- and radio-sensitizing properties.
Conclusions:
- LB100 shows considerable therapeutic potential for diverse cancer types.
- LB100's ability to sensitize cancer cells warrants further clinical investigation.
- Ongoing Phase 1 trials are expected to provide crucial data on LB100's safety and efficacy.
