ArticleBiochimica et biophysica acta2014
Stereospecific requirement of cholesterol in the function of the serotonin1A receptor.
Article in Biochimica et biophysica acta, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 72 citations in OpenAlex.
- The orientation of cholesterol's hydroxy group affects its membrane dynamics and intracellular transport.iScience · 2026Article
- Chemokine receptor activity is differentially regulated by membrane cholesterol.bioRxiv : the preprint server for biology · 2026Article
- Effects of Membrane Cholesterol on the Structure and Function of Selected Class A GPCRs─Challenges and Future Perspectives.Biochemistry · 2025Review
- Role of Cholesterol and its Biosynthetic Precursors on Membrane Organization and Dynamics: A Fluorescence Approach.The Journal of membrane biology · 2023Article
- PI(4,5)PAdvances in experimental medicine and biology · 2023Article
- Smith-Lemli-Opitz syndrome: A pathophysiological manifestation of the Bloch hypothesis.Frontiers in molecular biosciences · 2023Review
- Lysine 101 in the CRAC Motif in Transmembrane Helix 2 Confers Cholesterol-Induced Thermal Stability to the SerotoninThe Journal of membrane biology · 2022Article
- Cyclodextrins: Only Pharmaceutical Excipients or Full-Fledged Drug Candidates?Pharmaceutics · 2022Review
- Cholesterol-dependent endocytosis of GPCRs: implications in pathophysiology and therapeutics.Biophysical reviews · 2021Review
- A molecular sensor for cholesterol in the human serotoninScience advances · 2021Article
- Allosteric Modulation of GPCRs of Class A by Cholesterol.International journal of molecular sciences · 2021Review
- Major Depressive Disorder (MDD) and Antidepressant Medication Are Overrepresented in High-Dose Statin Treatment.Frontiers in medicine · 2021Article
- Structure and Dynamics of GPCRs in Lipid Membranes: Physical Principles and Experimental Approaches.Molecules (Basel, Switzerland) · 2020Review
- Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases.Journal of medicinal chemistry · 2020Article
- Effect of sterol structure on ordered membrane domain (raft) stability in symmetric and asymmetric vesicles.Biochimica et biophysica acta. Biomembranes · 2019Article
- Membrane cholesterol depletion reduces downstream signaling activity of the adenosine ABiochimica et biophysica acta. Biomembranes · 2019Article
- A Database of Predicted Binding Sites for Cholesterol on Membrane Proteins, Deep in the Membrane.Biophysical journal · 2018Article
- Stereospecific Interactions of Cholesterol in a Model Cell Membrane: Implications for the Membrane Dipole Potential.The Journal of membrane biology · 2018Article
- Effects of host cell sterol composition upon internalization ofThe Journal of biological chemistry · 2018Article
- Discrimination of Stereoisomers by Their Enantioselective Interactions with Chiral Cholesterol-Containing Membranes.Molecules (Basel, Switzerland) · 2017Article
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Authors and funding
6 authors at 3 institutions in 3 countries.
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Abstract
The serotonin1A receptor is an important member of the G protein-coupled receptor (GPCR) family. It is involved in the generation and modulation of a variety of cognitive and behavioral functions and serves as a drug target. Previous work from our laboratory has established the sensitivity of the function of the serotonin1A receptor to membrane cholesterol. Solubilization of the hippocampal serotonin1A receptor utilizing the zwitterionic detergent CHAPS is accompanied by loss of cholesterol and results in reduction in specific ligand binding. Replenishment of cholesterol to solubilized membranes restores specific ligand binding to the receptor. We utilized this strategy of sterol replenishment of solubilized membranes to explore the stereospecific stringency of cholesterol for receptor function. We used two stereoisomers of cholesterol, ent-cholesterol (enantiomer of cholesterol) and epi-cholesterol (a diastereomer of cholesterol), for this purpose. Importantly, we show here that while ent-cholesterol could replace cholesterol in supporting receptor function, epi-cholesterol could not. These results imply that the requirement of membrane cholesterol for the serotonin1A receptor function is diastereospecific, yet not enantiospecific. Our results extend and help define specificity of the interaction of membrane cholesterol with the serotonin1A receptor, and represent the first report utilizing ent-cholesterol to examine stereospecificity of GPCR-cholesterol interaction.
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Registered trials
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