Evidence map›Paper›PMID 20394377›Full record

ArticleJournal of medicinal chemistry2010

Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.

Enrica Calleri, Stefania Ceruti, Gloria Cristalli, Claudia Martini, Caterina Temporini, Chiara Parravicini, Rosaria Volpini, Simona Daniele, Gabriele Caccialanza, Davide Lecca and 8 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing 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

17 citing papers in PubMed, 71 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Preparation and characterization of immobilized 5-HTJournal of pharmaceutical and biomedical analysis · 2022
    Article
  5. Article
  6. Review
  7. Article
  8. Review
  9. Article
  10. Synthesis and Ability of New Ligands for G Protein-Coupled Receptors 17 (GPR17).Medical science monitor : international medical journal of experimental and clinical research · 2017
    Article
  11. Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Recent developments in protein-ligand affinity mass spectrometry.Analytical and bioanalytical chemistry · 2011
    Review
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

18 authors at 6 institutions in 2 countries.

Enrica CalleriDepartment of Pharmaceutical Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
Stefania Ceruti
Gloria Cristalli
Claudia Martini
Caterina Temporini
Chiara Parravicini
Rosaria Volpini
Simona Daniele
Gabriele Caccialanza
Davide Lecca
Catia Lambertucci
Maria Letizia Trincavelli
Gabriella Marucci
Irving W Wainer
Graziella Ranghino
Piercarlo Fantucci
Maria P Abbracchio
Gabriella Massolini
Università di Camerino · ITUniversity of Milan · ITUniversity of Pavia · ITUniversity of Pisa · ITNational Institute on Aging · USUniversity of Milano-Bicocca · IT

Funding

Immobilized Receptors In Drug DiscoveryZIAAG000295 · NIA · NATIONAL INSTITUTE ON AGING · PI EGAN, JOSEPHINE · 2009 to 2025
$11.4M
EXAMINING THE ROLE OF DACHSHUND IN MUSHROOM BODIESF30MH011912 · NIMH · BAYLOR COLLEGE OF MEDICINE · PI MARTINI, SHARYL R · 1998 to 2002
$76k
NIMH NIH HHS F30 MH011912
6 · The paper itself

Abstract

The application of frontal affinity chromatography-mass spectrometry (FAC-MS), along with molecular modeling studies, to the screening of potential drug candidates toward the recently deorphanized G-protein-coupled receptor (GPCR) GPR17 is shown. GPR17 is dually activated by uracil nucleotides and cysteinyl-leukotrienes, and is expressed in organs typically undergoing ischemic damage (i.e., brain, heart and kidney), thus representing a new pharmacological target for acute and chronic neurodegeneration. GPR17 was entrapped on an immobilized artificial membrane (IAM), and this stationary phase was used to screen a library of nucleotide derivatives by FAC-MS to select high affinity ligands. The chromatographic results have been validated with a reference functional assay ([(35)S]GTPgammaS binding assay). The receptor nucleotide-binding site was studied by setting up a column where a mutated GPR17 receptor (Arg255Ile) has been immobilized. The chromatographic behavior of the tested nucleotide derivatives together with in silico studies have been used to gain insights into the structure requirement of GPR17 ligands.

Indexed as

Binding SitesChromatography, AffinityHumansLigandsMass SpectrometryMembranes, ArtificialModels, MolecularNucleotidesProtein BindingReceptors, G-Protein-CoupledStructure-Activity RelationshipGPR17 protein, humanLigandsMembranes, ArtificialNucleotidesReceptors, G-Protein-Coupled

Identifiers

PMID20394377
PMCPMC6201305
OpenAlexW2009229514

What OpenQuestion holds

Textmetadata
LicenceTDM
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.