Sigma Receptors


Sigma-1 receptor agonists have been widely accepted for their antidepressant roles, and it is observed that most clinically successful SSRIs/SNRIs are sigma-1 receptor ligands. These agonists have also been found to be of interest to researchers studying Alzheimer’s and Parkinson’s.

Sigma-1 antagonists show great promise in the treatment of cancer, as they can shrink tumours while having no observable effect on their animal hosts. Antagonists are in clinical trials for the treatment of pain, with interesting data in both neuropathic and inflammatory pain. Recent findings also show positive results in the co-treatment of classical anticancer drugs with sigma-1 antagonists to treat tumours while affecting the pain associated with them.

Some of the above effects are linked to the roles played by sigma-1 ligands in regulating TRPV1, potassium, sodium, voltage-activated calcium channels, as well as inositol trisphosphate receptors.

An unrelated protein, the sigma-2 receptor, has been proposed for many years. Last year, a paper claiming it to be TMEM97 was published. While this is being assessed (we’ve been here before, to find that PGRMC-1 was NOT sigma-2), the interest in sigma-2 high. Sigma-2 binding site levels are high in tumours, and this has allowed development of diagnostic tools to detect tumours in vivo, as well as ligands that cause tumour cell death to be considered high value tools in oncology.

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Kathy Andrews
Managing Editor
Journal of Genomics & Gene Study