Evidence map›Paper›PMID 40884041›Full record

ArticleAngewandte Chemie (International ed. in English)2025

Potent Fluorescent Probe for Target-Engagement Studies of Allosteric Pyruvate Kinase Modulators.

Oscar Nilsson, Anna P Valaka, Liliana Håversen, Agnieszka Bogucka, István Köteles, Paul Brear, Mikael Rutberg, Anders Gunnarsson, Marko Hyvönen, Morten Grøtli

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Angewandte Chemie (International ed. in English), 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. Article
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.

Oscar NilssonDepartment of Chemistry and Molecular Biology, University of Gothenburg, Medicinaregatan 7B, Gothenburg, SE-413 90, Sweden.ORCID 0000-0003-2716-2563
Anna P ValakaDepartment of Chemistry and Molecular Biology, University of Gothenburg, Medicinaregatan 7B, Gothenburg, SE-413 90, Sweden.ORCID 0009-0008-7007-6971
Liliana HåversenDepartment of Molecular and Clinical Medicine, University of Gothenburg and Sahlgrenska University Hospital, Gothenburg, SE-413 45, Sweden.ORCID 0000-0001-5180-7830
Agnieszka BoguckaDepartment of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge, CB2 1GA, UK.ORCID 0000-0001-5317-4344
István KötelesDepartment of Chemistry and Molecular Biology, University of Gothenburg, Medicinaregatan 7B, Gothenburg, SE-413 90, Sweden.ORCID 0000-0002-1678-233X
Paul BrearDepartment of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge, CB2 1GA, UK.
Mikael RutbergDepartment of Molecular and Clinical Medicine, University of Gothenburg and Sahlgrenska University Hospital, Gothenburg, SE-413 45, Sweden.
Anders GunnarssonDiscovery Sciences, R&D Gothenburg, AstraZeneca, Mölndal, SE-431 83, Sweden.ORCID 0000-0002-6334-9520
Marko HyvönenDepartment of Biochemistry, University of Cambridge, 80 Tennis Court Road, Cambridge, CB2 1GA, UK.ORCID 0000-0001-8683-4070
Morten GrøtliDepartment of Chemistry and Molecular Biology, University of Gothenburg, Medicinaregatan 7B, Gothenburg, SE-413 90, Sweden.ORCID 0000-0003-3621-4222

Funding

Wellcome Trust
6 · The paper itself

Abstract

Pyruvate kinases (PKs) are highly allosterically regulated enzymes that play a central role in cellular metabolism and are increasingly recognized as valuable therapeutic targets in cancer, metabolic diseases, and diabetes. Despite their biological and clinical significance, methods to directly assess allosteric ligand engagement of PK isoforms remain limited. Here, we report the development of LumiPK, a novel, environment-sensitive fluorescent tracer designed to monitor allosteric binding to the liver isoform of pyruvate kinase (PKL). LumiPK integrates an environment-sensitive 4-sulfamonyl-7-aminobenzoxadiazole fluorophore into a potent allosteric modulator scaffold. It emerged as the lead compound from a small ligand series, showing high affinity for PKL (K

Indexed as

Fluorescent DyesPyruvate KinaseAllosteric RegulationHumansLigandsMolecular StructureFluorescent DyesLigandsPyruvate KinaseAllosterismBiological activityDrug discoveryFluorescent probesMedicinal chemistry

Identifiers

PMID40884041
PMCPMC12518693

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.