{"title":"Intracellular GPCR modulators enable precision pharmacology.","authors":"Brian E Krumm, Bryan L Roth","doi":"10.1038/s44386-025-00011-8","DOIUrl":null,"url":null,"abstract":"<p><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>","PeriodicalId":520448,"journal":{"name":"NPJ drug discovery","volume":"2 1","pages":"8"},"PeriodicalIF":0.0000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12069105/pdf/","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"NPJ drug discovery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1038/s44386-025-00011-8","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/5/12 0:00:00","PubModel":"Epub","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
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.
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