ArticleNature structural & molecular biology2022
Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119.
Article in Nature structural & molecular biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. 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, 56 citations in OpenAlex.
- Constitutive activity among orphan G protein-coupled receptors: Molecular mechanisms and pharmacological perspectives.Molecular pharmacology · 2026Review
- Multiomics Integration Reveals Rearing System-Induced Variations in Volatile Organic Compounds, Metabolites, and Meat Quality of Lueyang Black-Bone Chickens.Journal of agricultural and food chemistry · 2025Article
- Constitutively active orphan G protein-coupled receptors through the lenses of cryo-electron microscopy.The Journal of biological chemistry · 2025Review
- Molecular mechanism of pH sensing and activation in GPR4 reveals proton-mediated GPCR signaling.Cell discovery · 2025Article
- Molecular basis for ligand recognition and receptor activation of the prostaglandin D2 receptor DP1.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Article
- Structural basis of the cysteinyl leukotriene receptor type 2 activation by LTD4.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Lysophosphatidylcholine promoting α-Synuclein aggregation in Parkinson's disease: disrupting GCase glycosylation and lysosomal α-Synuclein degradation.NPJ Parkinson's disease · 2025Article
- Structural basis for lipid-mediated activation of G protein-coupled receptor GPR55.Nature communications · 2025Article
- Exploring the constitutive activation mechanism of the class A orphan GPR20.Acta pharmacologica Sinica · 2025Article
- Molecular mechanism of ligand recognition and activation of lysophosphatidic acid receptor LPAR6.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- The role of metabolites in the progression of osteoarthritis: Mechanisms and advances in therapy.Journal of orthopaedic translation · 2025Review
- Native mass spectrometry prescreening of G protein-coupled receptor complexes for cryo-EM structure determination.Structure (London, England : 1993) · 2024Article
- Review
- From Classical to Alternative Pathways of 2-Arachidonoylglycerol Synthesis: AlterAGs at the Crossroad of Endocannabinoid and Lysophospholipid Signaling.Molecules (Basel, Switzerland) · 2024Review
- The binding mechanism of an anti-multiple myeloma antibody to the human GPRC5D homodimer.Nature communications · 2024Article
- Constitutive activation mechanism of a class C GPCR.Nature structural & molecular biology · 2024Article
- Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor, GPR3.Biochemistry · 2024Article
- Lysophosphatidylcholines Enriched withACS medicinal chemistry letters · 2024Article
- Structural basis for lysophosphatidylserine recognition by GPR34.Nature communications · 2024Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors at 6 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Lysophosphatidylcholine (LPC) is an essential mediator in human lipid metabolism and is associated with a variety of diseases, but the exact identity of LPC receptors remains controversial. Through extensive biochemical and structural analyses, we have identified the orphan receptor GPR119 as the receptor for LPC. The structure of the GPR119-G-protein complex without any added ligands reveals a density map that fits well with LPC, which is further confirmed by mass spectrometry and functional studies. As LPCs are abundant on the cell membrane, their preoccupancy in the receptor may lead to 'constitutive activity' of GPR119. The structure of GPR119 bound to APD668, a clinical drug candidate for type 2 diabetes, reveals an exceedingly similar binding mode to LPC. Together, these data highlight structural evidence for LPC function in regulating glucose-dependent insulin secretion through direct binding and activation of GPR119, and provide structural templates for drug design targeting GPR119.
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.