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Direct Mechanisms in Cholesterol Modulation of Protein Function pp 89–103Cite as

Effects of Cholesterol on GPCR Function: Insights from Computational and Experimental Studies

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Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 1135))

Abstract

The extensive experimental and computational evidences revealed that cholesterol is involved in the drug binding to G protein-coupled receptor (GPCR) targets that is influenced by the membrane environment and external functions. These multifunctional factors make the understanding of the molecular mechanism of action in greater detail an entirely difficult task. Significant efforts have been made for better understanding the role of multi-directional specific, receptor-dependent interactions of cholesterol, and its effects on drug design and development. Additional efforts must be made in this complex system in order to shed more light on cholesterol molecular basis of action. The results of molecular simulations that complemented experimental data may reveal new aspects of GPCR-cholesterol interactions and may provide a comprehensive understanding of receptor function.

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Author information

Authors and Affiliations

  1. Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodistrian University of Athens, Athens, Greece

    Sofia Kiriakidi & Thomas Mavromoustakos

  2. Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Athens, Greece

    Antonios Kolocouris

  3. Department of Pharmacology, School of Medicine, University of Crete, Heraklion, Crete, Greece

    George Liapakis

  4. Computational Biology and Molecular Simulations Laboratory, Department of Biophysics, School of Medicine, Bahcesehir University, Istanbul, Turkey

    Saima Ikram & Serdar Durdagi

Authors
  1. Sofia Kiriakidi
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  2. Antonios Kolocouris
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  3. George Liapakis
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  4. Saima Ikram
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  5. Serdar Durdagi
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  6. Thomas Mavromoustakos
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Corresponding authors

Correspondence to Serdar Durdagi or Thomas Mavromoustakos .

Editor information

Editors and Affiliations

  1. Department of Chemistry, University of Illinois, Chicago, IL, USA

    Avia Rosenhouse-Dantsker

  2. Department of Pharmacology, The University of Tennessee HSC, Memphis, TN, USA

    Anna N. Bukiya

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Kiriakidi, S., Kolocouris, A., Liapakis, G., Ikram, S., Durdagi, S., Mavromoustakos, T. (2019). Effects of Cholesterol on GPCR Function: Insights from Computational and Experimental Studies. In: Rosenhouse-Dantsker, A., Bukiya, A. (eds) Direct Mechanisms in Cholesterol Modulation of Protein Function. Advances in Experimental Medicine and Biology, vol 1135. Springer, Cham. https://doi.org/10.1007/978-3-030-14265-0_5

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