Traditional medicines serve not only as an integral part of medical treatments prescribed by healthcare providers but also as a fundamental reservoir for novel molecular scaffolds. However, gaps remain in our understa...Traditional medicines serve not only as an integral part of medical treatments prescribed by healthcare providers but also as a fundamental reservoir for novel molecular scaffolds. However, gaps remain in our understanding of the mechanisms underlying their activity. A superfamily of membraneproteins, G protein-coupled receptors (GPCRs), have been demonstrated tobe potential targets for several compounds isolated from traditional medicines. Given that GPCRs serve as targets for approximately one-third of allmarketed drugs, they may be compelling targets for repurposing traditionalmedicines. Despite this potential, research investigating their activity or potential ligands across GPCRome, the library of human GPCRs, is scarce.Drawing on the functional and structural knowledge presently available,this review contemplates prospective trends in GPCR drug discovery, proposes innovative strategies for investigating traditional medicines, andhighlights ligand screening approaches for identifying novel drug-like molecules. To discover bioactive molecules from traditional medicines thateither directly bind to GPCRs or indirectly modify their function, a genomewide pan-GPCR drug discovery platform was designed for the identificationof bioactive components and targets, and the evaluation of their pharmacological profiles. This platform aims to aid the exploration of all-sided relations between traditional medicines and GPCRome using advanced highthroughput screening techniques. We present various approaches used bymany, including ourselves, to illuminate the previously unexplored aspectsof traditional medicines and GPCRs.展开更多
基金funded by introducing the talented person scientific research starts funds subsidization project of Chengdu University of Traditional Chinese Medicine(030040043,030040017).
文摘Traditional medicines serve not only as an integral part of medical treatments prescribed by healthcare providers but also as a fundamental reservoir for novel molecular scaffolds. However, gaps remain in our understanding of the mechanisms underlying their activity. A superfamily of membraneproteins, G protein-coupled receptors (GPCRs), have been demonstrated tobe potential targets for several compounds isolated from traditional medicines. Given that GPCRs serve as targets for approximately one-third of allmarketed drugs, they may be compelling targets for repurposing traditionalmedicines. Despite this potential, research investigating their activity or potential ligands across GPCRome, the library of human GPCRs, is scarce.Drawing on the functional and structural knowledge presently available,this review contemplates prospective trends in GPCR drug discovery, proposes innovative strategies for investigating traditional medicines, andhighlights ligand screening approaches for identifying novel drug-like molecules. To discover bioactive molecules from traditional medicines thateither directly bind to GPCRs or indirectly modify their function, a genomewide pan-GPCR drug discovery platform was designed for the identificationof bioactive components and targets, and the evaluation of their pharmacological profiles. This platform aims to aid the exploration of all-sided relations between traditional medicines and GPCRome using advanced highthroughput screening techniques. We present various approaches used bymany, including ourselves, to illuminate the previously unexplored aspectsof traditional medicines and GPCRs.
