lb-100 has been researched along with Neoplasms* in 2 studies
1 review(s) available for lb-100 and Neoplasms
| Article | Year |
|---|---|
LB100, a small molecule inhibitor of PP2A with potent chemo- and radio-sensitizing potential.
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. Topics: Animals; Antineoplastic Agents; Apoptosis; Bridged Bicyclo Compounds, Heterocyclic; Cell Cycle; Drug Evaluation, Preclinical; Drug Resistance, Neoplasm; Enzyme Inhibitors; Humans; Mitosis; Neoplasms; Oncogene Proteins; Piperazines; Protein Phosphatase 2; Radiation-Sensitizing Agents; Tumor Protein, Translationally-Controlled 1; Tumor Suppressor Proteins; Wnt Signaling Pathway | 2015 |
1 other study(ies) available for lb-100 and Neoplasms
| Article | Year |
|---|---|
The Antitumor Drug LB-100 Is a Catalytic Inhibitor of Protein Phosphatase 2A (PPP2CA) and 5 (PPP5C) Coordinating with the Active-Site Catalytic Metals in PPP5C.
LB-100 is an experimental cancer therapeutic with cytotoxic activity against cancer cells in culture and antitumor activity in animals. The first phase I trial (NCT01837667) evaluating LB-100 recently concluded that safety and efficacy parameters are favorable for further clinical testing. Although LB-100 is widely reported as a specific inhibitor of serine/threonine phosphatase 2A (PP2AC/ Topics: Amino Acid Sequence; Bridged Bicyclo Compounds, Heterocyclic; Catalysis; Catalytic Domain; Cell Line, Tumor; Humans; Metals; Methylation; Mutagenesis, Site-Directed; Neoplasms; Nuclear Proteins; Phosphoprotein Phosphatases; Piperazines; Protein Phosphatase 2 | 2019 |