WARF: P09097US02

Sigma 1 Receptor Inhibitors May Provide New Cancer, Psychosis, Addiction and Other Therapies


Arnold Ruoho, Abdol Hajipour, Uyen Chu, Dominique Fontanilla

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing new therapeutic compounds for the mammalian sigma 1 receptor, an important and undertargeted receptor that may be associated with cancer and neurological and cardiovascular disorders.
OVERVIEWThe sigma 1 receptor is an intracellular molecule that shares no known homology with any mammalian proteins. In the brain, sigma 1 receptors regulate the activity of ion channels via protein-protein interactions.

The activation of sigma 1 receptors may promote neuronal differentiation and interfere with programmed cell death, potentially leading to cancer. The sigma 1 receptor also has been implicated in other disorders, including psychosis, drug addiction and retinal degeneration. As a result, ligands for this receptor may provide a new class of therapeutic drugs. However, few ligands that inhibit the sigma 1 receptor are known, and those ligands have been poorly studied thus far.
THE INVENTIONUW-Madison researchers have discovered a new class of compounds that are high affinity inhibitors of the sigma 1 receptor. These compounds are cytotoxic against many cancer cell lines, including breast, lung, prostate, ovarian, colorectal and CNS. They could be used as antipsychotic agents, to treat cocaine addiction or cardiovascular disorders or to inhibit the growth of cancer cells.

The inventors characterized the sigma 1 receptor ligand binding regions to define novel and essential features of the molecular scaffold of high affinity ligands. They found that long chain alkylamines are a key feature of ligands, such as the fungicide tridemorph, that bind to the sigma 1 receptor with high affinity and inhibit its activity.
  • Treatment for neurological disorders, cancer or cardiovascular disorders
  • Provides new therapeutic leads for an important and undertargeted receptor
  • Because sigma 1 receptors are overexpressed in many tumor cell lines, ligands for this receptor may be used for imaging and treating cancer.
  • Selectively binds to the sigma 1 receptor rather than the sigma 2 receptor
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Contact Information
For current licensing status, please contact Rafael Diaz at or 608-960-9847.
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