Evidence map›Paper›PMID 40890559›Full record

ArticleEJNMMI research2025

Studies on the impact of modifications at the Gln-Trp site in RM2-based GRPR ligands.

Sebastian Fischer, Lena Koller, Sandra Dominelli, Roswitha Beck, Hans-Jürgen Wester, Thomas Günther

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in EJNMMI research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

6 authors.

Sebastian Fischer *TUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany.
Lena KollerTUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany.
Sandra DominelliTUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany.
Roswitha BeckTUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany.
Hans-Jürgen WesterTUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany.
Thomas Günther *TUM School of Natural Sciences, Department of Chemistry, Chair of Pharmaceutical Radiochemistry, Technical University of Munich, 85748, Garching, Germany. thomas.guenther@tum.de.ORCID http://orcid.org/0000-0002-7412-0297

Funding

Deutsche Forschungsgemeinschaft DFG - 68647618
6 · The paper itself

Abstract

backgroundOne of the most studied, and preclinically as well as clinically applied gastrin-releasing peptide receptor (GRPR) ligands represents the antagonist RM2 (DOTA-Pip

resultsGRPR affinity and lipophilicity of RM2 derivatives were in a range of 1.2-8.4 nM and - 2.9 to - 1.1 (

conclusionSubstitution of the Gln-Trp site in RM2 by artificial amino acids had a distinct impact on overall pharmacokinetics. While Hse (instead of Gln) and Bta (instead of Trp) led to a decreased, α-Me-Trp (instead of Trp) led to an increased in vivo stability, which resulted in improved pharmacokinetics over time in case of the latter. However, at 1 h post-injection both [

Indexed as

AntagonistGRPRMetabolic stabilityModified pharmacophoreRM2

Identifiers

PMID40890559
PMCPMC12401824

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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.