Evidence map›Paper›PMID 40775579›Full record

ArticleEJNMMI research2025

A preclinical study on the influence of linkers in [

Esther Olaniran Håkansson, Ivan V Zelepukin, Karim Obeid, Athanasios Bitzios, Ekaterina Bezverkhniaia, Amulya Sunkara, Ulrika Rosenström, Anna Orlova, Luke R Odell, Panagiotis Kanellopoulos

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Article in EJNMMI research, 2025. 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
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

10 authors.

Esther Olaniran Håkansson *Department of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Ivan V Zelepukin *Department of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Karim ObeidDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Athanasios BitziosDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Ekaterina BezverkhniaiaDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Amulya SunkaraDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Ulrika RosenströmDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Anna OrlovaDepartment of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.ORCID http://orcid.org/0000-0001-6120-2683
Luke R Odell *Department of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden.
Panagiotis Kanellopoulos *Department of Medicinal Chemistry, Uppsala University, Uppsala, 751 23, Sweden. Panagiotis.kanellopoulos@ilk.uu.se.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

backgroundGastrin-releasing peptide receptor (GRPR) is overexpressed in several cancers, including prostate and breast, making it an attractive target for radiopharmaceutical development. Studies on GRPR-targeting radioligands highlight the critical role of the spacer region between the GRPR-recognition motif and radiolabeled moiety, which can significantly influence peptide pharmacokinetics and pharmacodynamics. Herein, we investigated the impact of structurally restricted spacers on the performance of RM26-based radioligands.

resultsThree novel radioligands were designed to each bear a NOTA chelator via different spacers composed of N-acetyl-lysine followed by either o-ethyltoluene (oET), o-methylanisole (oMA), or m-methylanisole (mMA) motifs. The peptides were successfully labeled with Ga-68, achieving high radiochemical yield, purity, and molar activity. The resulting [

conclusionsAmong the three radioligands, the peptide bearing the N-acetyl-lysine-oET spacer exhibited the fastest background clearance and better PET imaging of prostate cancer xenografts. The incorporation of conformationally restricted spacers is a promising strategy for developing tracers with high GRPR binding and good imaging properties, but further optimization is necessary to reduce uptake in healthy tissues.

Indexed as

AntagonistBombesin analogueGRPRProstate cancerRadiopharmaceuticalsStructure-properties relationship

Identifiers

PMID40775579
PMCPMC12332157

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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.