Design Strategies for Bivalent Ligands Targeting GPCRs

  title={Design Strategies for Bivalent Ligands Targeting GPCRs},
  author={Jeremy Shonberg and P. Scammells and B. Capuano},
  • Jeremy Shonberg, P. Scammells, B. Capuano
  • Published 2011
  • Medicine, Chemistry
  • ChemMedChem
  • Specifically designed bivalent ligands targeting G protein‐coupled receptor (GPCR) dimeric structures have become increasingly popular in recent literature. The advantages of the bivalent approach are numerous, including enhanced potency and receptor subtype specificity. However, the use of bivalent ligands as potential pharmacotherapeutics is limited by problematic molecular properties, such as high molecular weight and lipophilicity. This Minireview focuses on the design of bivalent ligands… CONTINUE READING
    51 Citations

    Topics from this paper.

    Design of bivalent ligands targeting putative GPCR dimers.
    Bridging the gap: bitopic ligands of G-protein-coupled receptors.
    • 105
    Structure-guided development of heterodimer-selective GPCR ligands
    • 47
    • PDF
    The size matters? A computational tool to design bivalent ligands
    • 5
    • PDF
    GPCR crystal structures: Medicinal chemistry in the pocket.
    • 85


    Synthesis and evaluation of homo-bivalent GnRHR ligands.
    • 42
    Receptor dimerization--rationale for the design of bivalent ligands.
    • 17
    Multivalent-based drug design applied to serotonin 5-HT(4) receptor oligomers.
    • 14
    Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.
    • 55
    Rational design of dualsteric GPCR ligands: quests and promise
    • 91
    Orthosteric/allosteric bitopic ligands: going hybrid at GPCRs.
    • 63