Evidence map›Paper›PMID 28673732›Full record

ArticleBioorganic & medicinal chemistry2017

Design, synthesis and biological evaluation of GPR55 agonists.

Lara Fakhouri, Christopher D Cook, Mohammed H Al-Huniti, Linda M Console-Bram, Dow P Hurst, Michael B S Spano, Daniel J Nasrallah, Marc G Caron, Larry S Barak, Patricia H Reggio and 2 more

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Article
  6. Article
  7. Crosstalk between the MCellular signalling · 2020
    Review
  8. Article
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

12 authors.

Lara FakhouriDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Christopher D CookDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Mohammed H Al-HunitiDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Linda M Console-BramTemple University School of Medicine, Anatomy and Cell Biology, Center for Substance Abuse Research, 3420 North Broad St., Philadelphia, PA 19140, United States.
Dow P HurstDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Michael B S SpanoDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Daniel J NasrallahDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Marc G CaronDuke Center of Excellence, 444 Sands Building, Department of Cell Biology, Durham, NC 27710, United States.
Larry S BarakDuke Center of Excellence, 444 Sands Building, Department of Cell Biology, Durham, NC 27710, United States.
Patricia H ReggioDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Mary E AboodTemple University School of Medicine, Anatomy and Cell Biology, Center for Substance Abuse Research, 3420 North Broad St., Philadelphia, PA 19140, United States.
Mitchell P CroattDepartment of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States. Electronic address: mpcroatt@uncg.edu.

Funding

Pilot Projects Core (PPC)P30DA013429 · NIDA · TEMPLE UNIV OF THE COMMONWEALTH · PI Munir Gunes Kutlu · 2000 to 2026
$34.6M
Science PlanP30DA029925 · NIDA · DUKE UNIVERSITY · PI CARON, MARC G. · 2010 to 2018
$6.2M
Molecular Characterization of GPR35 and GPR55, Putative Cannabinoid ReceptorsR01DA023204 · NIDA · TEMPLE UNIV OF THE COMMONWEALTH · PI ABOOD, MARY E · 2007 to 2016
$3.2M
NIDA NIH HHS P30 DA013429NIDA NIH HHS P30 DA029925NIDA NIH HHS R01 DA023204
6 · The paper itself

Abstract

GPR55, a G protein-coupled receptor, is an attractive target to alleviate inflammatory and neuropathic pain and treat osteoporosis and cancer. Identifying a potent and selective ligand will aid to further establish the specific physiological roles and pharmacology of the receptor. Towards this goal, a targeted library of 22 compounds was synthesized in a modular fashion to obtain structure-activity relationship information. The general route consisted of coupling a variety of p-aminophenyl sulfonamides to isothiocyanates to form acylthioureas. For the synthesis of a known naphthyl ethyl alcohol motif, route modification led to a shorter and more efficient process. The 22 analogues were analyzed for their ability to serve as agonists at GPR55 and valuable information for both ends of the molecule was ascertained.

Indexed as

Drug DesignDose-Response Relationship, DrugHumansMolecular StructureReceptors, CannabinoidReceptors, G-Protein-CoupledStructure-Activity RelationshipThioureaGPR55 protein, humanReceptors, CannabinoidReceptors, G-Protein-CoupledThioureaCancerGPR55Homology modelThioureaβ-Arrestin recruitment assay

Identifiers

PMID28673732
PMCPMC5752104

What OpenQuestion holds

Textmetadata
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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.