Evidence map›Paper›PMID 19022181›Full record

ArticleChemistry & biology2008

Ligand-binding architecture of human CB2 cannabinoid receptor: evidence for receptor subtype-specific binding motif and modeling GPCR activation.

Ying Pei, Richard W Mercier, Jenine K Anday, Ganesh A Thakur, Alexander M Zvonok, Dow Hurst, Patricia H Reggio, David R Janero, Alexandros Makriyannis

Abstract read
In one paragraph

Article in Chemistry & biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 53 papers.

0numbers the graph read from it
0cells of the map it votes in
53citing papers in PubMed
3.0field-weighted citation impact, top 9% of its field
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

53 citing papers in PubMed, 101 citations in OpenAlex.

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  12. Covalent Inhibition of the Histamine HMolecules (Basel, Switzerland) · 2019
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

9 authors at 3 institutions in 1 country.

Ying PeiSchool of Pharmacy, University of Connecticut, Storrs, CT 06269, USA.
Richard W Mercier
Jenine K Anday
Ganesh A Thakur
Alexander M Zvonok
Dow Hurst
Patricia H Reggio
David R Janero
Alexandros Makriyannis
Northeastern University · USUniversity of Connecticut · USUniversity of North Carolina at Greensboro · US

Funding

Project 3 - In vivo pharmacology of cannabinoid receptor probesP01DA009158 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI Alexandros Makriyannis · 1994 to 2026
$26.0M
Molecular Determinants of Cannabinoid ActivityR01DA003934 · NIDA · UNIVERSITY OF NORTH CAROLINA GREENSBORO · PI REGGIO, PATRICIA HODAPP · 1985 to 2019
$5.6M
MOLECULAR BASIS OF CANNABINOID ACITIVITYR37DA003801 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI MAKRIYANNIS, ALEXANDROS · 1997 to 2006
$3.7M
MOLECULAR BASIS OF CANNABINOID ACTIVITYR01DA003801 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI MAKRIYANNIS, ALEXANDROS · 1985 to 2017
$2.5M
Interactions of endocannabinoids and nicotinic receptorsZ01DA000489 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI LUPICA, CARL · 2006 to 2008
$611k
MOLECULAR DETERMINANTS FOR CANNABINOID ACTIVITYK02DA000489 · NIDA · UNIVERSITY OF NORTH CAROLINA GREENSBORO · PI REGGIO, PATRICIA HODAPP · 2000 to 2004
$530k
Intramural NIH HHS Z01 DA000489NIDA NIH HHS DA03934NIDA NIH HHS DA3801NIDA NIH HHS DA9158NIDA NIH HHS K02 DA000489NIDA NIH HHS P01 DA009158NIDA NIH HHS R01 DA003801NIDA NIH HHS R01 DA003934NIDA NIH HHS R37 DA003801
6 · The paper itself

Abstract

The extensive physiological influence of transmission through the CB2 cannabinoid receptor makes this G protein-coupled receptor (GPCR) a promising therapeutic target for treating neuropathic pain, inflammation, and immune disorders. However, there is little direct structural information pertaining to either GPCR or CB2-receptor ligand recognition and activation. The present work helps characterize experimentally the ligand-binding interactions of the human CB2 (hCB2) receptor. This study illustrates how our overall experimental approach, "ligand-assisted protein structure" (LAPS), affords direct determination of the requirements for ligand binding to the hCB2 receptor and discrimination among the binding motifs for ligands that activate therapeutically relevant GPCRs.

Indexed as

Models, MolecularAffinity LabelsAmino Acid SequenceCell LineDrug DiscoveryGene Expression RegulationHumansLigandsMolecular Sequence DataMutagenesis, Site-DirectedMutant ProteinsMutationProtein BindingReceptor, Cannabinoid, CB1Receptor, Cannabinoid, CB2Substrate SpecificityAffinity LabelsLigandsMutant ProteinsReceptor, Cannabinoid, CB1Receptor, Cannabinoid, CB2

Identifiers

PMID19022181
PMCPMC3700404
OpenAlexW2011754496

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

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.