G-Protein-Coupled Receptors as Therapeutic Targets for CNS Disorders
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".
Deadline for manuscript submissions: 27 March 2026
Special Issue Editors
Interests: medicinal chemistry; drug discovery; GPCR ligands; structure-activity relationship studies; bioactive compounds
Special Issues, Collections and Topics in MDPI journals
Interests: drug discovery; receptor ligands; structure-activity relationship studies; bioactive compounds
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
G-protein-coupled receptors (GPCRs) represent the largest family of membrane receptors in the human genome and play pivotal roles in cellular signaling across various physiological systems. In the central nervous system (CNS), GPCRs are critical for regulating neurotransmitter release, synaptic plasticity, neuronal excitability, and neuroinflammation. Accumulating evidence has highlighted the strong relationship between GPCR dysfunction and the pathophysiology of numerous CNS disorders, including schizophrenia, depression, anxiety, Parkinson’s disease, Alzheimer’s disease, and epilepsy. Moreover, there is growing evidence linking GPCRs to brain cancer development, in particular glioblastoma tumor progression. Advances in GPCR structural biology and biased signaling have opened up new avenues for the development of functionally selective ligands that offer improved efficacy and reduced side effects. Another cutting-edge approach is the development of positive or negative allosteric modulators (PAMs or NAMs), which increase receptor subtype selectivity and preserve the spatial and temporal dynamics of physiological signaling, crucial for complex CNS functions. Additionally, targeting GPCR heteromers endowed with unique signaling properties and implicated in disease-specific brain circuits offers a new layer of specificity. Finally, the multitarget approach, combining different GPCR systems, might produce improved results in the treatment of polyfactorial CNS pathologies. In this Special Issue, authors are invited to submit original articles dealing with the discovery and/or development of subtype selective or multitarget ligands targeting GPCRs that are potentially useful for the treatment of CNS diseases. Review articles focusing on recent findings in this area of investigation will also be welcome.
Dr. Fabio Del Bello
Dr. Wilma Quaglia
Guest Editors
Manuscript Submission Information
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Keywords
- GPCRs
- CNS disorders
- biased ligands
- allosteric modulators
- GPCR heteromers
- multitarget ligands
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