Evidence map›Paper›PMID 42861104›Full record

ArticleBiochemistry and biophysics reports2026

Development of a GPCR-binding ligand screening method using real-time interaction analysis on live cells.

Hadis Westin, Hanna Yushchyshyna, Olga Vorontsova, Saloni Chopra, Tianqi Xu, Christoffer Bengtsson, Fabio Begnini, Preeti Jha, Ulrika Rosenström, Ulrika Yngve and 2 more

Abstract read
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In one paragraph

Article in Biochemistry and biophysics reports, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0cells of the map it votes in
0citing papers in PubMed
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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.

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

12 authors.

Hadis WestinRidgeview Instruments AB, Uppsala, Sweden.
Hanna YushchyshynaDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Olga VorontsovaDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Saloni ChopraDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Tianqi XuDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Christoffer BengtssonDrug Discovery and Development Platform, SciLifeLab, Sweden.
Fabio BegniniDrug Discovery and Development Platform, SciLifeLab, Sweden.
Preeti JhaDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Ulrika RosenströmDepartment of Medicinal Chemistry, Uppsala University, Uppsala, Sweden.
Ulrika YngveDrug Discovery and Development Platform, SciLifeLab, Sweden.
Marika NestorDepartment of Immunology, Genetics and Pathology, SciLifeLab, Uppsala University, Uppsala, Sweden.
Jos BuijsRidgeview Instruments AB, Uppsala, Sweden.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

G protein-coupled receptors (GPCRs) affect many physiological processes and frequently used as drug targets and biomarkers. The present study focuses on the neurokinin 1 receptor (NK1-R) which is over-expressed on neural tumours with the aim to develop high affinity binders to NK1-R for theranostic purposes. 60 Ligands were synthesized, all containing iodine enabling isotopic exchange with radioactive iodine for imaging or radiotherapeutic applications. Embedded in the cellular membrane, GPCRs adopt various conformational states that can change upon interaction with ligands. Therefore, a time-resolved, live cell assay was developed to evaluate competition with fluorescently labelled endogenous NK1-R ligand, Substance P (FAM-SP). The time resolved assay enabled quantification of the efficiency in which the ligands compete for the rapid and slow releasing NK1-R binding modes of FAM-SP. Of the 60 ligands, 25 were able to displace FAM-SP faster than the anti-nausea drug aprepitant. Two of these ligands displaced the rapid releasing FAM-SP fraction faster than Substance P (SP) and one of them also replaced the slow releasing fraction faster than aprepitant. To validate the assay, the affinity of two ligands for several NK1-R expressing cell lines was further quantified; one that had similar competition characteristics as SP and one that behaved as aprepitant. The ligand with similar competition characteristics as SP displayed a low nM to sub-pM affinity with a stronger binding correlating with higher receptor expression levels. This high affinity makes it a highly promising candidate for further development into a theranostic agent to address neural tumours.

Indexed as

Binding affinityGPCR ligand interactionsLive-cell screening assayNeurokinin 1 receptor (NK1-R)Receptor binding kineticsTargeted radiotherapyTheranostic ligand

Identifiers

PMID42861104
PMCPMC13653987

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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.