G protein-coupled receptors (GPCRs) form the cornerstone of cellular communication and physiological regulation, representing one of the largest and most versatile families of cell surface receptors. Their pivotal role in mediating numerous pathophysiological processes positions them as prime targets in drug discovery and development. Despite considerable advancements, the complex signaling mechanisms and multifaceted functions of GPCRs still pose significant research challenges and opportunities for innovation. Current questions center around understanding the intricate molecular mechanisms, receptor dynamics, and their implications in diverse disease contexts.

Recent studies have provided profound insights into the structural and functional aspects of GPCRs, advancing our understanding of ligand-receptor interactions, allosteric modulation, and biased signaling. These discoveries are fueled by innovative techniques such as cryo-electron microscopy and advanced computational modeling, opening new avenues for drug design and therapeutic interventions targeting GPCRs. However, despite significant progress, the quest for clinical translation remains, requiring more in-depth exploration of GPCR signaling pathways and their potential in overcoming therapeutic resistance.

This Research Topic aims to summarize the latest findings in GPCR and receptor pharmacology, elucidating the molecular underpinnings and therapeutic implications of GPCR signaling. We seek to uncover novel insights that could bridge the gap between basic pharmacological research and clinical application. To gather further insights in GPCR regulation and therapeutic targeting, we welcome articles addressing, but not limited to, the following themes:

o Structural and functional analyses of GPCRs and their ligand interactions

o Insights into allosteric modulation and biased signaling

o Advances in computational modeling and drug design targeting GPCRs

o Cutting-edge technologies for studying receptor pharmacology in physiological and pathological conditions

o Novel therapeutics targeting GPCRs and their clinical implications in disease management

o Role of GPCR signaling in disease pathogenesis and resistance to therapy

We invite original research articles, reviews, and perspective pieces that highlight innovative approaches and emerging trends in the field of GPCR and receptor pharmacology. Together, we strive to foster collaboration and knowledge exchange that accelerates discoveries in experimental pharmacology and drug discovery.

Please note that submissions lacking experimental validation of in silico findings will not be considered.

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Decoding GPCR Functionality: Bridging Molecular Pharmacology and Drug Discovery