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<p>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.</p>

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Intracellular GPCR modulators enable precision pharmacology

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年5月12日

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  • Brian E. Krumm,
  • Bryan L. Roth

摘要

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.