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cis-Urocanic acid
- Development stage
- Phase 2
- Lead developer
- Herantis Pharma
- Modality
- Small Molecules
- Administration
- Intravesical
01
Overview
cis-Urocanic acid is a small molecule derivative of the amino acid histidine, formed in mammalian skin from trans-urocanic acid upon exposure to ultraviolet radiation. It acts as a protodynamic agent with potential anti-inflammatory and antiproliferative activity. Upon intravesical instillation, it becomes protonated in the mildly acidic extracellular tumor environment and penetrates cancer cells; inside the more alkaline cytosol, it releases protons that increase intracellular acidity. This process impairs cellular metabolic activity and can lead to cell cycle arrest and apoptosis or necrosis. Additionally, cis-urocanic acid enhances ERK and JNK signaling by inhibiting serine/threonine and tyrosine phosphatases. It is also an immune modulator that induces immunosuppression by binding as an agonist to the serotonin 5-HT2A receptor.
- Other names
- Imidazole-4-acrylic acid (Z)cis-Urocanic acid
02
Targets
HTR2A (Serotonin receptor 5-HT2A)
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