ArticleNature chemical biology2012
Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands.
Article in Nature chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 84 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
84 citing papers in PubMed, 198 citations in OpenAlex.
- Safety, Sedative, and Anxiolytic Evaluation of MECS Hard Capsules Using In Silico and In Vivo Approaches.ACS omega · 2026Article
- Exploring the role of zolpidem in alleviating cognitive and motor impairments in chronic cerebral hypoperfusion: a rat model study with in vivo and in silico insights.Experimental animals · 2026Article
- From 2-Azido Products to Complex Nitrogen Heterocycles: The Versatile Ugi MCR in Modern Synthesis.Current organic synthesis · 2026Article
- Assessment of Sedative Activity of Lonicerin: In Vivo Approach With Pharmacokinetics and Molecular Docking.Brain and behavior · 2025Article
- Neurosteroids: a lifelong impact on brain health.Frontiers in behavioral neuroscience · 2025Review
- Evaluating chemical effects on human neural cells through calcium imaging and deep learning.iScience · 2024Article
- Paradigm shift required for translational research on the brain.Experimental & molecular medicine · 2024Review
- Synthesis, In Vivo Anticonvulsant Activity Evaluation and In Silico Studies of Some Quinazolin-4(3H)-One Derivatives.Molecules (Basel, Switzerland) · 2024Article
- Ligand- and Structure-based Approaches for Transmembrane Transporter Modeling.Current drug research reviews · 2024Review
- Structure-function Studies of GABA (A) Receptors and Related computer-aided Studies.Journal of molecular neuroscience : MN · 2023Review
- Neurosteroid influence on affective tone.Neuroscience and biobehavioral reviews · 2023Review
- Article
- Article
- Allosteric crosstalk in modular proteins: Function fine-tuning and drug design.Computational and structural biotechnology journal · 2023Review
- Why won't it stop? The dynamics of benzodiazepine resistance in status epilepticus.Nature reviews. Neurology · 2022Review
- Pharmacological activation of ATF6 remodels the proteostasis network to rescue pathogenic GABACell & bioscience · 2022Article
- Long-term diazepam treatment enhances microglial spine engulfment and impairs cognitive performance via the mitochondrial 18 kDa translocator protein (TSPO).Nature neuroscience · 2022Article
- Insect RDL Receptor Models for Virtual Screening: Impact of the Template Conformational State in Pentameric Ligand-Gated Ion Channels.ACS omega · 2022Article
- Design, Synthesis, and Evaluation of Anticonvulsant Activities of New Triazolopyrimidine Derivatives.Frontiers in chemistry · 2022Article
- Carbon Dots Derived from Os Draconis and Their Anxiolytic Effect.International journal of nanomedicine · 2022Article
24 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 2 institutions in 1 country.
Funding
Abstract
Benzodiazepines exert their anxiolytic, anticonvulsant, muscle-relaxant and sedative-hypnotic properties by allosterically enhancing the action of GABA at GABA(A) receptors via their benzodiazepine-binding site. Although these drugs have been used clinically since 1960, the molecular basis of this interaction is still not known. By using multiple homology models and an unbiased docking protocol, we identified a binding hypothesis for the diazepam-bound structure of the benzodiazepine site, which was confirmed by experimental evidence. Moreover, two independent virtual screening approaches based on this structure identified known benzodiazepine-site ligands from different structural classes and predicted potential new ligands for this site. Receptor-binding assays and electrophysiological studies on recombinant receptors confirmed these predictions and thus identified new chemotypes for the benzodiazepine-binding site. Our results support the validity of the diazepam-bound structure of the benzodiazepine-binding pocket, demonstrate its suitability for drug discovery and pave the way for structure-based drug design.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.