Evidence map›Paper›PMID 25769518›Full record

ArticleBioorganic & medicinal chemistry2015

Development of a time-resolved fluorescence probe for evaluation of competitive binding to the cholecystokinin 2 receptor.

N G R Dayan Elshan, Thanuja Jayasundera, Craig S Weber, Ronald M Lynch, Eugene A Mash

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 95% 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

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

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

5 authors at 1 institution in 1 country.

N G R Dayan ElshanDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721-0041, USA.
Thanuja JayasunderaDepartment of Physiology, University of Arizona, Tucson, AZ 85724-5051, USA.
Craig S WeberDepartment of Physiology, University of Arizona, Tucson, AZ 85724-5051, USA.
Ronald M LynchDepartment of Physiology, University of Arizona, Tucson, AZ 85724-5051, USA; The Bio5 Institute, University of Arizona, Tucson, AZ 85721-0240, USA.
Eugene A MashDepartment of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721-0041, USA. Electronic address: emash@email.arizona.edu.
University of Arizona · US

Funding

VITAMIN AP30CA023074 · NCI · UNIVERSITY OF ARIZONA · PI Dan Theodorescu · 1985 to 2026
$110.2M
Multimeric Ligands for Targeting of MelanomaR01CA097360 · NCI · UNIVERSITY OF ARIZONA · PI HRUBY, VICTOR J, MORSE, DAVID L · 2003 to 2012
$5.5M
Targeting Pancreatic CancerR01CA123547 · NCI · UNIVERSITY OF ARIZONA · PI MORSE, DAVID L · 2007 to 2011
$3.0M
Multimeric Ligands for Targeting of Pancreatic CancerR33CA095944 · NCI · UNIVERSITY OF ARIZONA · PI GILLIES, ROBERT J. · 2003 to 2005
$1.6M
Multimeric Ligands for Targeting of Pancreatic CancerR21CA095944 · NCI · UNIVERSITY OF ARIZONA · PI GILLIES, ROBERT J · 2002 to 2002
$152k
NCI NIH HHS P30 CA023074NCI NIH HHS P30 CA23074NCI NIH HHS R01 CA097360NCI NIH HHS R01 CA123547NCI NIH HHS R01 CA97360NCI NIH HHS R21 CA095944NCI NIH HHS R33 CA095944NCI NIH HHS R33 CA95944
6 · The paper itself

Abstract

The synthesis, characterization, and use of Eu-DTPA-PEGO-Trp-Nle-Asp-Phe-NH2 (Eu-DTPA-PEGO-CCK4), a luminescent probe targeted to cholecystokinin 2 receptor (CCK2R, aka CCKBR), are described. The probe was prepared by solid phase synthesis. A Kd value of 17±2nM was determined by means of saturation binding assays using HEK-293 cells that overexpress CCK2R. The probe was then used in competitive binding assays against Ac-CCK4 and three new trivalent CCK4 compounds. Repeatable and reproducible binding assay results were obtained. Given its ease of synthesis, purification, receptor binding properties, and utility in competitive binding assays, Eu-DTPA-PEGO-CCK4 could become a standard tool for high-throughput screening of compounds in development targeted to cholecystokinin receptors.

Indexed as

Binding, CompetitiveFluorescent DyesHEK293 CellsHumansReceptor, Cholecystokinin BSpectrometry, FluorescenceFluorescent DyesReceptor, Cholecystokinin BCholecystokinin 2 receptorDissociation-enhanced lanthanide fluoroimmunoassayHigh-throughput screeningMultivalent bindingTime-resolved fluorescence

Identifiers

PMID25769518
PMCPMC4380538
OpenAlexW2010185757

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.