Regulation of alpha-1B adrenergic receptor localization, trafficking, function, and stability

Myron L. Toews, Steven C. Prinster, Nancy A. Schulte

Research output: Contribution to journalArticlepeer-review

22 Scopus citations


The alpha-1 adrenergic receptors (α1ARs) play important roles in normal physiology and in many disease states, and understanding their signaling pathways and regulatory mechanisms is thus of considerable relevance, in particular for identifying pharmacological targets for therapeutic modulation. The expression, function, localization, trafficking, and stability of these receptors are all subject to complex regulation by diverse molecular mechanisms. This article highlights recent studies from our laboratory and others focused on the localization and trafficking of the alpha-1B adrenergic receptor (α1BAR) subtype and on changes in its stability that are likely to be involved in regulating receptor expression. The role(s) of protein kinase C in α1BAR sequestration, endocytosis, and extracellular signal-regulated kinase (ERK) activation are summarized, and evidence for α1BAR localization in caveolae/rafts is presented. Receptor structural domains involved in the multiple steps and mechanisms of agonist-induced desensitization are described. Finally, aspects of α 1BAR structural stability that appear to control its drug-induced up- and down-regulation are discussed. Our understanding of regulation for the α1BAR subtype provides a model for studies of the differential regulation of the other α1AR subtypes and may lead to identification of new molecular targets for therapeutic intervention in a variety of disease states.

Original languageEnglish (US)
Pages (from-to)379-389
Number of pages11
JournalLife Sciences
Issue number2-3
StatePublished - Dec 5 2003


  • Alpha-1 adrenergic receptor
  • Caveolae
  • Desensitization
  • Down-regulation
  • Endocytosis
  • Extracellular signal-regulated kinase
  • G protein coupling
  • Inherent instability
  • Internalization
  • Protein kinase C
  • Sequestration
  • Site-directed mutagenesis
  • Up-regulation

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)


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