Cellular and Molecular Biology of Orphan G Protein-Coupled Receptors

Da Young Oh, Kyungjin Kim, Hyuk Bang Kwon, Jae Young Seong

    Research output: Chapter in Book/Report/Conference proceedingChapter

    48 Citations (Scopus)

    Abstract

    The superfamily of G protein-coupled receptors (GPCRs) is the largest and most diverse group of membrane-spanning proteins. It plays a variety of roles in pathophysiological processes by transmitting extracellular signals to cells via heterotrimeric G proteins. Completion of the human genome project revealed the presence of ∼168 genes encoding established nonsensory GPCRs, as well as 207 genes predicted to encode novel GPCRs for which the natural ligands remained to be identified, the so-called orphan GPCRs. Eighty-six of these orphans have now been paired to novel or previously known molecules, and 121 remain to be deorphaned. A better understanding of the GPCR structures and classification; knowledge of the receptor activation mechanism, either dependent on or independent of an agonist; increased understanding of the control of GPCR-mediated signal transduction; and development of appropriate ligand screening systems may improve the probability of discovering novel ligands for the remaining orphan GPCRs.

    Original languageEnglish
    Title of host publicationA Survey of Cell Biology
    EditorsJeon Kwang
    Pages163-218
    Number of pages56
    DOIs
    Publication statusPublished - 2006

    Publication series

    NameInternational Review of Cytology
    Volume252
    ISSN (Print)0074-7696

    Keywords

    • Agonist
    • Antagonist
    • Constitutive activity
    • Deorphaned
    • G protein-coupled receptor
    • Ligand
    • Orphan
    • Screening assay
    • Signaling

    ASJC Scopus subject areas

    • Histology
    • Cell Biology

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