Dual-Action Kinase Modulators: A Novel Therapeutic Class for Cancer and Fibrotic Diseases
This invention introduces a novel class of small molecule compounds designed to modulate critical cellular signaling pathways, specifically activating the AMPK enzyme and inhibiting Epithelial-Mesenchymal Transition (EMT) drivers. This dual-action mechanism targets the fundamental processes underlying cell proliferation, metastasis, and tissue remodeling, offering a powerful new therapeutic strategy for a wide range of diseases including cancer and organ fibrosis.
Description
The novel compounds function by directly activating the Adenosine Monophosphate-activated Protein Kinase (AMPK), a master regulator of cellular energy balance known for its tumor-suppressive and anti-fibrotic roles. Crucially, the compounds also act as a common inhibitor of the three major signaling cascades that drive EMT: the Hippo, Wnt, and TGF beta pathways. The innovative aspect lies in this unique, dual-targeting strategy. The compound activates tumor suppressor kinases (AMPK and Mst/Lats), which in turn engages a degradation complex to eliminate EMT-inducing transcription factors like TAZ. By simultaneously controlling metabolic function and suppressing these pro-metastatic and pro-fibrotic signaling pathways, the technology is positioned to halt cancer progression, reverse organ scarring, and provide a treatment for various metabolic disorders.Applications
- Oncology treatment- Treatment of other fibrotic or metabolic diseases
- Metabolic and Age-Related Diseases
- Combinatorial Cancer Therapy (adjuvant therapy)
- Inflammatory and Pain Disorders
Advantages
- Broad Therapeutic Potential: Addresses multiple major disease classes including oncology, fibrotic disorders, and metabolic diseases via a common mechanism.- Inhibits Core Disease Drivers: Functions as a common inhibitor of the three main pathways (Hippo, Wnt, TGF beta) responsible for Epithelial-Mesenchymal Transition (EMT).
- Novel Anti-Cancer Efficacy: Demonstrated ability to significantly inhibit cancer cell migration and proliferation across different malignant cell lines.
- Enhances Chemotherapy Response: Shown to increase the sensitivity of cancer cells to standard chemotherapeutics, offering a path to overcome drug resistance.
- Metabolically Active: Potently activates AMPK, linking the therapeutic action to the regulation of glucose/lipid metabolism and promoting cellular housekeeping.