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Orphan GPR52 as an emerging neurotherapeutic target
Saghir Ali1, Pingyuan Wang1, Ryan E Murphy1
1Chemical Biology Program, Department of Pharmacology and Toxicology, and Center for Addiction Sciences and Therapeutics, University of Texas Medical Branch, Galveston, TX 77555, USA.
Drug Discovery Today
|February 22, 2024
Summary
G protein-coupled receptor 52 (GPR52) plays a role in neurological diseases. Targeting GPR52 offers potential therapeutic strategies for conditions like schizophrenia and Huntington's disease.
Area of Science:
- Neuroscience
- Pharmacology
- Molecular Biology
Background:
- G protein-coupled receptor 52 (GPR52) is a conserved, brain-enriched receptor.
- It is coupled to Gs/olf proteins and influences cyclic AMP (cAMP) signaling.
- GPR52 is implicated in various physiological and pathological brain processes.
Purpose of the Study:
- To review the current knowledge on GPR52 receptor distribution, structure, and functions.
- To highlight recent advancements in the discovery of small-molecule GPR52 ligands.
- To discuss the therapeutic potential and challenges of targeting GPR52.
Main Methods:
- Literature review of GPR52 research.
- Analysis of drug discovery efforts for GPR52 ligands.
- Discussion of clinical trial progress for GPR52-targeting drugs.
Main Results:
- GPR52 activity modulation may treat schizophrenia and Huntington's disease.
- An orally available GPR52 agonist (HTL0048149) is in phase I clinical trials for schizophrenia.
- Significant progress has been made in identifying small-molecule GPR52 ligands.
Conclusions:
- GPR52 is a promising therapeutic target for neurological and psychiatric disorders.
- Further research and drug development are needed to overcome challenges in targeting GPR52.
- Targeting GPR52 holds potential for novel treatments in human neurological diseases.
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