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Cholesterol and lipid phases influence the interactions between serotonin receptor agonists and lipid bilayers

Batchelor, Rebecca; Windle, Christopher J.; Buchoux, Sébastien; Lorch, Mark

Authors

Rebecca Batchelor

Christopher J. Windle

Sébastien Buchoux



Abstract

Solid state NMR techniques have been used to investigate the effect that two serotonin receptor 1a agonists (quipazine and LY-165,163) have on the phase behavior of, and interactions within, cholesterol/phosphocholine lipid bilayers. The presence of agonist, and particularly LY-165,163, appears to widen the phase transitions, an effect that is much more pronounced in the presence of cholesterol. It was found that both agonists locate close to the cholesterol, and their interactions with the lipids are modulated by the lipid phases. As the membrane condenses into mixed liquid-ordered/disordered phases, quipazine is pushed up toward the surface of the bilayer, whereas LY-165,163 moves deeper into the lipid chain region. In light of our results, we discuss the role of lipid/drug interactions on drug efficacy.

Citation

Batchelor, R., Windle, C. J., Buchoux, S., & Lorch, M. (2010). Cholesterol and lipid phases influence the interactions between serotonin receptor agonists and lipid bilayers. Journal of Biological Chemistry, 285(53), 41402-41411. https://doi.org/10.1074/jbc.M110.155176

Journal Article Type Article
Acceptance Date Oct 8, 2010
Online Publication Date Oct 20, 2010
Publication Date Dec 31, 2010
Deposit Date Nov 13, 2014
Journal Journal Of Biological Chemistry
Print ISSN 0021-9258
Publisher American Society for Biochemistry and Molecular Biology
Peer Reviewed Peer Reviewed
Volume 285
Issue 53
Pages 41402-41411
DOI https://doi.org/10.1074/jbc.M110.155176
Keywords Cell Biology; Biochemistry; Molecular Biology
Public URL https://hull-repository.worktribe.com/output/463426
Contract Date Nov 13, 2014