ArticleBioorganic & medicinal chemistry letters2011
Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.
Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Inhibition of autotransporter biogenesis by small molecules.Molecular microbiology · 2019Article
- Exploring G Protein-Coupled Receptors (GPCRs) Ligand Space via Cheminformatics Approaches: Impact on Rational Drug Design.Frontiers in pharmacology · 2018Review
- A Role for Fragment-Based Drug Design in Developing Novel Lead Compounds for Central Nervous System Targets.Frontiers in neurology · 2015Review
- Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.ACS medicinal chemistry letters · 2013Article
- Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands.Journal of medicinal chemistry · 2012Article
- Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands.Nature chemical biology · 2012Article
- Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.Journal of medicinal chemistry · 2011Article
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Authors and funding
14 authors.
Funding
Abstract
A fragment library was screened against the G protein-coupled histamine H(4) receptor (H(4)R) and the ligand-gated ion channel serotonin 5-HT(3A) (5-HT(3A)R). Interestingly, significant overlap was found between H(4)R and 5-HT(3A)R hit sets. The data indicates that dual active H(4)R and 5 HT(3A)R fragments have a higher complexity than the selective compounds which has important implications for chemical genomics approaches. The results of our fragment-based library screening study illustrate similarities in ligand recognition between H(4)R and 5-HT(3A)R and have important consequences for selectivity profiling in ongoing drug discovery efforts on H(4)R and 5-HT(3A)R. The affinity profiles of our fragment screening studies furthermore match the chemical properties of the H(4)R and 5-HT(3A)R binding sites and can be used to define molecular interaction fingerprints to guide the in silico prediction of protein-ligand interactions and structure.
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