Invention:
DYRK1A has been implicated in multiple disease states, including Alzheimer's Disease and Down Syndrome. Researchers have discovered a new chemotype that has been exemplified with significant DYRK1A activity and have developed brain-penetrant small molecule DYRK1A inhibitors toward Alzheimer's and the cognitive deficits of Down Syndrome. Future research will further exemplify and evaluate behavior across the kinome. This comprehensive approach aims to develop potent and selective compounds that can selectively target DYRK1A, offering potential therapeutic interventions for diseases associated with DYRK1A dysregulation.
Background:
There is an urgent need for effective therapies for neurodegenerative diseases, such as Alzheimer’s Disease and Down Syndrome, which are characterized by cognitive decline and lack adequate treatment options. Current technologies in this field involve extensive screening of chemical libraries, virtual screening, and structure-based drug design to identify potential inhibitors. However, these approaches can be time-consuming, costly, and may result in low success rates in identifying inhibitors with desired potency and selectivity. Furthermore, the translation of identified inhibitors into clinically viable drugs faces challenges, such as optimizing drug-like properties and addressing off-target effects. The disclosed technology aims to improve on these issues by offering a more efficient and effective approach for the discovery of novel DYRK1A inhibitors.
Applications:
- Treatment for Alzheimer's Disease
- Down Syndrome (DS) therapy
- Cancer research
Advantages:
- Targeted therapeutic
- Potential for disease modification
- Personalized medicine
