Ferrostatins for therapeutic control of reactive oxygen species in excitotoxic and degenerative diseasesTechnology #cu14077
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Programmed cell death is essential for homeostasis but may also contribute to disabling neuronal pathologies. Four genetically distinct mechanisms of cell death are known: apoptosis, autophagy, necrosis, and ferroptosis. Ferroptosis has been found to cause excitotoxic and degenerative damage to neurons. Importantly, Ferrostatin-1 (Fer-1) is a potent inhibitor of ferroptosis and has prevented cell death in in vitro models of Huntington’s disease, periventricular leukomalacia and kidney dysfunction. Following this success, analogs of Fer-1 were created, focusing on optimizing the compound’s stability and solubility thereby making it a more viable therapeutic candidate. This technology is a set of Fer-1 derivatives, one of which, SRS 15-72, was found to have physical properties compatible with pharmaceutical preparation, making it a promising therapeutic candidate for pathologies that include ferroptosis.
Stable and soluble ferroptosis inhibitor treats disease by modulating lipid peroxidation
Fer-1 prevents glutamate-induced excitotoxicity in rat brain samples, as well as ferroptopic cell death in cancerous tissue and various neurodegenerative disease models including Huntington’s disease. Structure-activity relationship experiments following Fer-1 led to the synthesis of SRS 15-72 which has comparable potency while exhibiting increased stability and solubility in vitro. Altogether, this technology has the potential to be a potent tool in the fight against degenerative diseases involving lipid peroxidation such as amyotrophic lateral sclerosis, Huntington’s disease, and Parkinson’s disease.
- Small molecule therapeutic for degenerative disease
- Prophylaxis for neurodegeneration
- Probe for studying ferroptosis and neurodegeneration
- Method of modulating ferroptotic activity
- Method of modulating cell life spans
- Method of modulating iron metabolism
- New approach to antioxidant therapy
- Microsomal stability and solubility confirmed in vitro
- Based on compound with demonstrated in vitro effectiveness
- Inhibits ferroptosis, a cell-death mechanism involved in various neurodegenerative diseases.
Patent Pending (US 20160297748)
Patent Pending (WO/2015/084749)
Patent Pending (WO/2013/152039)
Tech Ventures Reference: IR CU14077