Technology ID
TAB-3600
Novel ALDH1A1 (aldehyde dehydrogenase 1 family member A1) Inhibitors for the Treatment of Cancer
E-Numbers
E-214-2014-0
Lead Inventor
Vasiliou, Vasilis
Lead IC
NCATS
Co-Inventors
Simeonov, Anton
Jadhav, Ajit
Yang, Shyh-Ming
Maloney, David
Yasgar, Adam
Lal, Madhu
Chen, Ying
Miller, Bettina
Messersmith, Wells
Arcaroli, John
Jimeno, Antonio
Thompson, David
ICs
NCATS
Applications
Therapeutics
Research Materials
Therapeutic Areas
Oncology
This technology includes the identification and use of novel inhibitors of ALDH1A1 (aldehyde dehydrogenase 1 family member A1) for the treatment of multiple diseases, including cancer, inflammation, and obesity. ALDH1A1 is an enzyme that has a role in alcohol metabolism, and has been implicated in maintaining cancer stem cells. A high-throughput screen was conducted that identified novel ALDH1A1 inhibitors. Medicinal chemistry optimization led to the identification of two chemical series with high potency, selectivity, and favorable ADME (absorption, distribution, metabolism, and excretion) properties.
Commercial Applications
Further clinical work with the novel inhibitors could support the indication of these novel ALDH1A1 inhibitors for a variety of indications including but not limited to cancer, inflammation, and obesity.
Competitive Advantages
The compounds of this series represent the most potent, selective, and drug-like inhibitors of ALDH1A 1 described to date.
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