10. Specific and Nonspecific Regulation of GPCR Function by Cholesterol

  1. Irena Levitan2 and
  2. Francisco J. Barrantes3
  1. Gerald Gimpl and
  2. Katja Gehrig-Burger

Published Online: 22 JUN 2012

DOI: 10.1002/9781118342312.ch10

Cholesterol Regulation of Ion Channels and Receptors

Cholesterol Regulation of Ion Channels and Receptors

How to Cite

Gimpl, G. and Gehrig-Burger, K. (2012) Specific and Nonspecific Regulation of GPCR Function by Cholesterol, in Cholesterol Regulation of Ion Channels and Receptors (eds I. Levitan and F. J. Barrantes), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118342312.ch10

Editor Information

  1. 2

    Department of Medicine, University of Illinois at Chicago, Chicago, IL, USA

  2. 3

    Facultad de Ciencias Médicas, Pontificia Universidad Católica Argentina, Aires, Argentina

Author Information

  1. Department of Biochemistry, Johannes Gutenberg-University of Mainz, Mainz, Germany

Publication History

  1. Published Online: 22 JUN 2012
  2. Published Print: 16 JUL 2012

ISBN Information

Print ISBN: 9780470874325

Online ISBN: 9781118342312

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Keywords:

  • GPCR function by cholesterol, specific and nonspecific regulation;
  • heptahelical GPCRs, forming the largest receptor superfamily;
  • cholesterol-binding motifs, for checking for GPCRs;
  • cholesterol content in living cells, cholesterol–MβCD as donors, for depleted cells;
  • cyclodextrin-based exchanges, membrane protein cholesterol specificity by SAR

Summary

This chapter contains sections titled:

  • Introduction

  • Presence of Cholesterol-Binding Domains?

  • Presence of Cholesterol-Rich Microdomains?

  • Alterations in Protein Function Induced by Changes in the Cholesterol Content in Membranes/Cells?

  • Alterations in Receptor Function, Following Substitution of Cholesterol by Sterol Analogs? Correlation of Receptor Function with Membrane Parameters, E.G., Membrane Fluidity?

  • Cholesterol-Binding Molecules as Functional “Cholesterol Competitors”?

  • Cholesterol Requirement for Heterologous (OVER) Expression, Solubilization, and Purification of Receptors?

  • Direct Interaction of the Receptor with Labeled Cholesterol Probes?

  • Concluding Remarks

  • References