About this Research Topic
The British Pharmacological Society held its annual meeting last December - Pharmacology 17 hosted a symposium on sigma-1 receptors. We would like to bring together publications based on this meeting with others from the field of sigma receptor research to highlight the diverse nature of sigma ligands and the areas they can be used in. This will be of wide interest to “Frontiers…” readers.
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.
An Research Topic issue of Frontiers in Pharmacology focusing on sigma receptors will aid cross-fertilisation of research and ideas on these proteins in a wide area of scientific disciplines.
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.
An Research Topic issue of Frontiers in Pharmacology focusing on sigma receptors will aid cross-fertilisation of research and ideas on these proteins in a wide area of scientific disciplines.
Keywords: Sigma-1, sigma-2, cancer, pain, depression
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