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Related Experiment Videos

Orphan seven transmembrane receptor screening.

M J Wigglesworth1, L A Wolfe, A Wise

  • 1Screening and Compound Profiling, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW Essex, UK. Mark.J.Wigglesworth@gsk.com

Ernst Schering Foundation Symposium Proceedings
|August 21, 2007
PubMed
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Identifying natural ligands for orphan seven transmembrane receptors (7TMRs) is key for drug discovery. This review explores methods to find these ligands, unlocking future therapeutic potential.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Genomics

Background:

  • Seven transmembrane receptors (7TMRs) are a major drug target class, with over 35% of marketed drugs targeting them.
  • The 7TMR superfamily comprises ~720 genes, with half encoding potential drug targets, yet ~155 remain orphan receptors with unknown ligands.
  • Deorphanizing these receptors is crucial for validating new drug targets and understanding disease associations.

Purpose of the Study:

  • To review methodologies for identifying natural ligands for orphan 7TMRs.
  • To provide case studies exemplifying these ligand identification strategies.
  • To highlight the potential of orphan 7TMRs for future drug discovery.

Main Methods:

  • Experimental screening of small molecule and peptide libraries.

Related Experiment Videos

  • Reverse pharmacology approaches.
  • Bioinformatic prediction of candidate ligands.
  • Deorphanization through natural ligand identification.

    • Main Results:

    • Established methodologies for identifying ligands at orphan 7TMRs are presented.
    • Case studies illustrate the successful application of these techniques.
    • The review consolidates knowledge on orphan 7TMR ligand discovery.

    Conclusions:

    • Identifying ligands for orphan 7TMRs is a critical step in drug discovery.
    • Diverse methodologies exist to facilitate the deorphanization of these receptors.
    • Unlocking the potential of orphan 7TMRs promises novel therapeutic avenues.