Technology ID
TAB-3593
Identification and Use of 12/15-Lipoxygenase (LOX) Inhibitors for Post-Strike Treatment
E-Numbers
E-088-2016-0
Lead Inventor
Van Leyen, Klaus (Harvard Medical School)
Co-Inventors
Holman, Theodore (University of California, Santa Cruz)
Maloney, David (NCATS)
Rai Bantukallu, Ganesha (NCATS)
Jadhav, Ajit (NCATS)
Simeonov, Anton (NCATS)
Applications
Therapeutics
Research Materials
Therapeutic Areas
Neurology
Lead IC
NCATS
ICs
NCATS
This technology includes the identification and use of 12/15-lipoxygenase (LOX) inhibitors, including ML351 and related analogs, for post-stroke treatment. The 12/15-LOX directly oxidizes lipid membranes leading to their direct attack. After a stroke, the activity of 12/15-LOX is upregulated and is thought to contribute to increased neuronal loss and blood-brain barrier leakage. A high-throughput screen was undertaken to find inhibitors, which were then subjected to medical chemistry optimization.
Commercial Applications
Further clinical work on the compounds described in this technology could lead to a potential treatment post-stroke to limit brain injury. These compounds have potential use with other neurodegenerative conditions.
Competitive Advantages
Identification of LOX inhibitors has been difficult because many of the inhibitors found have been antioxidants with low selectivity and low potency. The identified ML351-based compounds have been used in human and mouse studies and found to be potent and selective LOX inhibitors.
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