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Future Directions in GPCR Biased Signaling and Ligand Pharmacology
Dannya Estau1, Zijian Li2,3
1Department of Cardiology and Institute of Vascular Medicine, Peking University Third Hospital; Beijing Key Laboratory of Cardiovascular Receptors Research, State Key Laboratory of Vascular Homeostasis and Remodeling, and NHC Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides, Peking University; Research Unit of Medical Science Research Management/Basic and Clinical Research of Metabolic Cardiovascular Diseases, Chinese Academy of Medical Sciences, Peking University, Beijing, China.
None:
G protein-coupled receptor (GPCR) biased signaling has emerged as a transformative paradigm, reshaping both fundamental understanding of receptor biology and pharmacological intervention. Significant advances have been made in deciphering the mechanisms underlying biased signaling and in the development of ligands that selectively engage specific pathways. Here, we outline key future directions in GPCR biased signaling and ligand pharmacology including the biased signaling theories, structural insights, methodological innovations and ligand pharmacology theories. We hope that these perspectives will contribute to pharmacological research, drug R & D, and clinical drug research and promoting safer and more effective GPCR-targeted treatments for human diseases.
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