Evidence map›Paper›PMID 25881832›Full record

ArticleBioorganic & medicinal chemistry letters2015

The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.

James B Thomas, Angela M Giddings, Srinivas Olepu, Robert W Wiethe, Keith R Warner, Philippe Sarret, Jean-Michel Longpre, Scott P Runyon, Brian P Gilmour

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 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
0.3field-weighted citation impact, top 47% 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, 2 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

9 authors at 2 institutions in 2 countries.

James B ThomasCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States. Electronic address: jbthomas@rti.org.
Angela M GiddingsCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
Srinivas OlepuCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
Robert W WietheCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
Keith R WarnerCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
Philippe SarretDepartment of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12th Ave. North, Sherbrooke, QC J1H 5N4, Canada.
Jean-Michel LongpreDepartment of Pharmacology and Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12th Ave. North, Sherbrooke, QC J1H 5N4, Canada.
Scott P RunyonCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
Brian P GilmourCenter for Drug Discovery, RTI International, PO Box 12194, Research Triangle Park, NC 27709, United States.
RTI International · USUniversité de Sherbrooke · CA

Funding

Synthesis and Testing of Targeted Libraries to Identify Small-molecule Agonists aR33DA029961 · NIDA · RESEARCH TRIANGLE INSTITUTE · PI GILMOUR, BRIAN P, THOMAS, JAMES B. · 2012 to 2014
$1.5M
Synthesis and Testing of Targeted Libraries to Identify Small-molecule Agonists aR21DA029961 · NIDA · RESEARCH TRIANGLE INSTITUTE · PI GILMOUR, BRIAN P, THOMAS, JAMES B. · 2010 to 2011
$937k
NIDA NIH HHS DA029961NIDA NIH HHS R21 DA029961NIDA NIH HHS R33 DA029961
6 · The paper itself

Abstract

Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesia in relevant preclinical models. The amide bond in nonpeptide NTS1 antagonists plays a central role in receptor recognition and molecular conformation. Using NTS2 FLIPR and binding assays, we found that it is also a key molecular structure for binding and calcium mobilization at NTS2. We found that reversed amides display a shift from agonist to antagonist activity and provided examples of the first competitive nonpeptide antagonists observed in the NTS2 FLIPR assay. These compounds will be valuable tools for determining the role of calcium signaling in vitro to NTS2 mediated analgesia.

Indexed as

AmidesBiological AssayCalcium SignalingDose-Response Relationship, DrugLigandsMolecular StructurePainProtein BindingReceptors, NeurotensinAmidesLigandsReceptors, NeurotensinFLIPR assayNeurotensinNTRC-660NTRC-739NTS2 receptorPainSR48692

Identifiers

PMID25881832
PMCPMC4418200
OpenAlexW2060100865

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.