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Structural Basis for Chemerin Recognition and Signaling Through Its Receptors
Yezhou Liu1, Aijun Liu1,2, Richard D Ye1,3
1Kobilka Institute of Innovative Drug Discovery, School of Medicine, The Chinese University of Hong Kong, Shenzhen 518172, China.
Biomedicines
|November 27, 2024
Summary
Chemerin, a key adipokine, signals through G protein-coupled receptors (GPCRs) like CMKLR1 and GPR1. Structural insights reveal how chemerin interacts with these receptors, influencing cellular processes and GPCR evolution.
Area of Science:
- Biochemistry
- Structural Biology
- Molecular Pharmacology
Background:
- Chemerin is a chemotactic adipokine involved in adipogenesis, leukocyte chemotaxis, and neuroinflammation.
- Chemerin signals via G protein-coupled receptors (GPCRs), primarily CMKLR1 and GPR1, while CCRL2 acts as a binding protein.
- Recent advancements in structural biology have provided high-resolution structures for two chemerin receptors.
Purpose of the Study:
- To review the structural perspectives of chemerin receptors.
- To emphasize the structure-activity relationship in chemerin-receptor interactions.
- To compare chemerin receptors with other peptide-ligand GPCRs to understand their distinct features and evolution.
Main Methods:
- Analysis of high-resolution structures of chemerin receptors.
- Structure-activity relationship studies focusing on ligand recognition and G protein activation.
- Comparative analysis of chemerin receptors with other GPCRs.
Main Results:
- Detailed structural insights into chemerin receptors (CMKLR1 and GPR1).
- Identification of key receptor components involved in chemerin binding and signaling.
- Understanding conformational changes upon ligand binding that lead to G protein activation.
- Comparison highlighting shared and distinct features of chemerin receptors within the GPCR superfamily.
Conclusions:
- Structural biology provides critical understanding of chemerin receptor function.
- Structure-activity correlations illuminate mechanisms of chemerin signaling and GPCR activation.
- Comparative structural analysis aids in understanding GPCR evolution and subclass diversification.
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