ArticleBritish journal of pharmacology2024
Direct measurements of neurosteroid binding to specific sites on GABA
Article in British journal of pharmacology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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Who cites it
3 citing papers in PubMed.
- Neuroactive steroids in the programming of neurodevelopment: implications of maternal obesity.Frontiers in endocrinology · 2025Review
- Stereospecific Properties and Intracellular Transport of Novel Intrinsically Fluorescent Neurosteroids.ACS chemical neuroscience · 2024Article
- Subthreshold Cannabidiol Potentiates Levetiracetam in the Kainic Acid Model of Temporal Lobe Epilepsy: A Pilot Study.Pharmaceuticals (Basel, Switzerland) · 2024Article
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Authors and funding
12 authors.
Funding
Abstract
background and purposeNeurosteroids are allosteric modulators of GABA EXPERIMENTAL APPROACH: Two methods were developed to measure neurosteroid binding affinity: (1) quenching of specific tryptophan residues in neurosteroid binding sites by the neurosteroid 17-methylketone group, and (2) FRET between MQ290 (an intrinsically fluorescent neurosteroid) and tryptophan residues in the binding sites. The assays were developed using ELIC-α1GABA KEY
resultsAllopregnanolone (3α-OH neurosteroid) was shown to bind at intersubunit and intrasubunit sites with equal affinity, whereas epi-allopregnanolone (3β-OH neurosteroid) binds at the intrasubunit site. MQ290 formed a strong FRET pair with W246, acting as a site-specific probe for the intersubunit site. The affinity and site-specificity of several neurosteroid agonists and inverse agonists was measured using the MQ290 binding assay. The FRET assay distinguishes between competitive and allosteric inhibition of MQ290 binding and demonstrated an allosteric interaction between the two neurosteroid binding sites. CONCLUSIONS AND IMPLICATIONS: The affinity and specificity of neurosteroid binding to two sites in the ELIC-α1GABA
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