Chapter Eighteen - Novel Screening Paradigms for the Identification of Allosteric Modulators and/or Biased Ligands for Challenging G-Protein-Coupled Receptors

• Autores: Stephan Schann, Pascal Neuville, Michel Bouvier
• Localización: Annual reports in medicinal chemistry, ISSN 0065-7743, Vol 49, 2014, págs. 285-300
• Idioma: inglés
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• Resumen

  • Abstract GPCRs have proven to be a valuable target family for drug discovery with more than 30% of marketed drugs acting through this receptor superfamily. However, numerous members remain challenging with no selective and druggable ligands being successfully developed. For these difficult targets, novel strategies consisting in developing allosteric modulators (AMs), biased ligands (BLs), or antibodies (Abs) are now emerging. These new classes of ligands are associated with advantages for the development of safer therapeutics but their identification can also prove to be challenging and novel screening paradigms are required. This JOURter discusses these novel approaches for AM and BL identification and the recent identification of Abs showing AM/BL properties. Taken together, these new paradigms mark the beginning of a new GPCR drug discovery age.