Krumm Brian E, Roth Bryan L
Department of Pharmacology, School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC USA.
National Institute of Mental Health Psychoactive Drug Screening Program (NIMH PDSP), School of Medicine, University of North Carolina at Chapel Hill, Chapel Hill, NC USA.
NPJ Drug Discov. 2025;2(1):8. doi: 10.1038/s44386-025-00011-8. Epub 2025 May 12.
G-protein-coupled receptors (GPCRs) have proven to be the most successful target class for drug discovery but their complicated signal transduction pathways cause difficulties for drug development. Recently, ligands have been identified that engage an intracellular binding site which promotes pathway biased signal in cooperation with orthosteric ligands. Here, we explore the topic of biased signaling and intracellular modulators to understand their application for precision pharmacology of Class A or Rhodopsin-Like GPCRs.
G蛋白偶联受体（GPCRs）已被证明是药物研发中最成功的靶点类型，但其复杂的信号转导途径给药物开发带来了困难。最近，已鉴定出一些配体，它们与细胞内结合位点结合，与正构配体协同促进偏向性信号传导途径。在此，我们探讨偏向性信号传导和细胞内调节剂这一主题，以了解它们在A类或视紫红质样GPCRs精准药理学中的应用。
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