Current Advances in Therapeutic Potential of Sigma Receptor Ligands
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: 25 March 2025 | Viewed by 694
Special Issue Editors
Interests: medicinal chemistry; synthesis; anticancer; analgesia; hybrid compounds; statistical analysis
Interests: medicinal chemistry; cancer; databases; QSAR; chemical synthesis; radioligand binding assay; sigma receptor
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Although nearly 50 years have passed since their first description as opioid receptors, the field of sigma receptors continues to pique considerable interest. Both proteins predominantly localize in the endoplasmic reticulum and are considered orphan receptors, with implications spanning over a diverse range of conditions. The sigma-1 receptor exhibits a trimeric architecture, and it works as a chaperone protein at the endoplasmic reticulum−mitochondria interface, regulating Ca2+ signaling and cell survival. The sigma-1 receptor agonists show neuroprotective, antiamnestic, and antidepressant effects, while the antagonists have modulatory effects on opioid analgesia, alongside antiproliferative and antiangiogenic activities.
The molecular identity of the sigma-2 receptor has more recently been determined as TMEM97, a regulator of the sterol transporter NPC1. The sigma-2 receptor is found in lungs, liver, and kidney, and it is highly expressed in several malignant tumors.
These findings suggest the potential of pharmacological modulation of sigma receptors to yield useful drugs across various conditions. In this context, the present special issue aims to collect both original research articles and comprehensive reviews concerning the development of sigma receptor ligands and associated efforts toward their therapeutic applications.
Dr. Maria Dichiara
Dr. Emanuele Amata
Guest Editors
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Keywords
- sigma-1 receptor
- sigma-2 receptor
- TMEM97
- cancer, neurodegeneration
- neuroprotection
- pain
- CNS disorders
- SAR
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