ArticleNature chemical biology2017
Orphan receptor ligand discovery by pickpocketing pharmacological neighbors.
Article in Nature chemical biology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It has been retracted, and should not be counted. Cited by 30 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
30 citing papers in PubMed, 48 citations in OpenAlex.
- Pharmacological proximities in the GPCR family discovered using contact-informed amino-acid and binding pocket similarities.bioRxiv : the preprint server for biology · 2026Article
- An in silico framework to visualize how cancer-associated mutations influence structural plasticity of the chemokine receptor CCR3.Protein science : a publication of the Protein Society · 2025Article
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- Orphan G Protein-Coupled Receptor GPR37 as an Emerging Therapeutic Target.ACS chemical neuroscience · 2023Review
- Building the Chordata Olfactory Receptor Database using more than 400,000 receptors annotated by Genome2OR.Science China. Life sciences · 2022Article
- G Protein Coupled Receptors Potentially Involved in Oligodendrogenesis: A Gene Expression Analysis.Iranian journal of public health · 2022Article
- Metabolic Profiling of Mice with Deletion of the Orphan G Protein-Coupled Receptor, GPR37L1.Cells · 2022Article
- The Structural Basis of Peptide Binding at Class A G Protein-Coupled Receptors.Molecules (Basel, Switzerland) · 2021Review
- Expression of the G protein-coupled receptor (GPR) 37 and GPR37L1 in the mouse digestive system.The Journal of veterinary medical science · 2021Article
- Benchmarking GPCR homology model template selection in combination with de novo loop generation.Journal of computer-aided molecular design · 2020Article
- Common activation mechanism of class A GPCRs.eLife · 2019Article
- Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs.Nature structural & molecular biology · 2019Review
- Computational advances in combating colloidal aggregation in drug discovery.Nature chemistry · 2019Review
- Constitutively active BRS3 is a genuinely orphan GPCR in placental mammals.PLoS biology · 2019Article
- G protein-coupled receptor 37L1 regulates renal sodium transport and blood pressure.American journal of physiology. Renal physiology · 2019Article
- GPR35 promotes glycolysis, proliferation, and oncogenic signaling by engaging with the sodium potassium pump.Science signaling · 2019Article
- GPCR homology model template selection benchmarking: Global versus local similarity measures.Journal of molecular graphics & modelling · 2019Article
- Article
- The Orphan Receptor GPR35 Contributes to Angiotensin II-Induced Hypertension and Cardiac Dysfunction in Mice.American journal of hypertension · 2018Article
Corrections and comments
- Retraction · 2021-03-01Doing the Right Thing · Error in Methods · Error in Results and/or Conclusions · · see also: https://www.nature.com/articles/s41589-021-00748-z
- Retracted
Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
Abstract
Understanding the pharmacological similarity of G protein-coupled receptors (GPCRs) is paramount for predicting ligand off-target effects, drug repurposing, and ligand discovery for orphan receptors. Phylogenetic relationships do not always correctly capture pharmacological similarity. Previous family-wide attempts to define pharmacological relationships were based on three-dimensional structures and/or known receptor-ligand pairings, both unavailable for orphan GPCRs. Here, we present GPCR-CoINPocket, a novel contact-informed neighboring pocket metric of GPCR binding-site similarity that is informed by patterns of ligand-residue interactions observed in crystallographically characterized GPCRs. GPCR-CoINPocket is applicable to receptors with unknown structure or ligands and accurately captures known pharmacological relationships between GPCRs, even those undetected by phylogeny. When applied to orphan receptor GPR37L1, GPCR-CoINPocket identified its pharmacological neighbors, and transfer of their pharmacology aided in discovery of the first surrogate ligands for this orphan with a 30% success rate. Although primarily designed for GPCRs, the method is easily transferable to other protein families.
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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.