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Using Receptor Antagonists in Binding Studies to Characterize a Mammalian Endothelin Receptor

  • J. Ruth Wu-Wong
Protocol
Part of the Methods in Molecular Biology™ book series (MIMB, volume 206)

Abstract

Endothelin (ET) is a peptide with 21-amino acid residues (1). Three distinct members of the ET family, namely, ET-1, ET-2 and ET-3, have been identified in humans through cloning (2). The effects of ETs on mammalian organs and cells are initiated by their binding to G-protein-linked receptors found in various tissues and cells (3). Two types of mammalian ET receptors, ETA and ETB, have been characterized, purified (4,5), and their cDNA have been cloned (6,7). ETA receptors are selective for ET-1 and ET-2, while ETB receptors bind ET-1, ET-2 and ET-3 with equal affinity. In addition, an ET receptor specific for ET-3 (termed ETc receptor or ETcR) was cloned from Xenopus laevis dermal melanophores (8). Although pharmacological studies suggest that there may be more endothelin receptor subtypes (9), no additional homologous mammalian cDNAs other than ETA and ETB have been identified.

Keywords

Binding Buffer Binding Study Scatchard Analysis Dissociation Rate Constant Antagonist Binding 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Humana Press Inc. 2002

Authors and Affiliations

  • J. Ruth Wu-Wong
    • 1
  1. 1.Abbott LaboratoriesSanta Clara

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