Evidence map›Paper›PMID 42720487›Full record

ArticleJournal of medicinal chemistry2026

Small-Molecule Activators of PRMT1: Discovery, SAR Analyses, and Proapoptotic Effects in Pancreatic Cancer Cells.

Sepideh Salehipour-Bavarsad, Christian Iking, Jonas Kammertöns, Caroline Bouchard, Marion Meixner, Michael Daude, Wieland Steinchen, Felix Terwesten, Johanna Senst, David Vonhören and 17 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2026. 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

27 authors.

Sepideh Salehipour-BavarsadPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Christian IkingPhilipps-Universität Marburg, Department of Medicinal Chemistry, Center for Tumor and Immune Biology (ZTI), Hans-Meerwein-Str. 3, Marburg35043, Germany.
Jonas KammertönsPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.
Caroline BouchardPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Marion MeixnerPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Michael DaudePhilipps-Universität Marburg, Department of Medicinal Chemistry, Center for Tumor and Immune Biology (ZTI), Hans-Meerwein-Str. 3, Marburg35043, Germany.
Wieland SteinchenPhilipps-Universität Marburg, Center for Synthetic Microbiology (SYNMIKRO), Karl-von-Frisch-Str. 14, 35043Marburg, Germany.
Felix TerwestenPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.
Johanna SenstPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.
David VonhörenPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Sinja RakowPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Anne KagerhuberPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Sona MartirosianPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.
Katrin RothPhilipps-Universität Marburg, Imaging Core Facility, Center for Tumor Biology and Immune Biology, Hans-Meerwein-Str. 3, Marburg35043, Germany.
Daniel HilgerPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.
Stefanie DörrPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.
Gina BachPhilipps-Universität Marburg, Department of Medicinal Chemistry, Center for Tumor and Immune Biology (ZTI), Hans-Meerwein-Str. 3, Marburg35043, Germany.
Van Tuan TrinhPhilipps-Universität Marburg , Department of Chemistry, Hans-Meerwein-Str. 4, Marburg35043, Germany.
Anett HauserPhilipps-Universität Marburg , Department of Chemistry, Hans-Meerwein-Str. 4, Marburg35043, Germany.
Frank AbendrothPhilipps-Universität Marburg , Department of Chemistry, Hans-Meerwein-Str. 4, Marburg35043, Germany.ORCID 0000-0002-0320-2690
Olalla VázquezPhilipps-Universität Marburg, Center for Synthetic Microbiology (SYNMIKRO), Karl-von-Frisch-Str. 14, 35043Marburg, Germany.ORCID 0000-0002-7555-1865
Gert BangePhilipps-Universität Marburg, Center for Synthetic Microbiology (SYNMIKRO), Karl-von-Frisch-Str. 14, 35043Marburg, Germany.
Jörg Walter BartschUniversity Hospital Marburg, Department of Neurosurgery, Baldingerstraße, Marburg35043, Germany.
Detlef Klaus BartschUniversity Hospital Marburg, Department of Visceral, Thoracic and Vascular Surgery, Baldingerstraße, Marburg35043, Germany.ORCID 0000-0003-1608-2496
Peter KolbPhilipps-Universität Marburg, Institute of Pharmaceutical Chemistry, Marbacher Weg 8, Marburg35032, Germany.ORCID 0000-0003-4089-614X
Wibke E DiederichPhilipps-Universität Marburg, Department of Medicinal Chemistry, Center for Tumor and Immune Biology (ZTI), Hans-Meerwein-Str. 3, Marburg35043, Germany.ORCID 0000-0001-5671-6575
Uta-Maria BauerPhilipps-Universität Marburg , Institute for Molecular Biology and Tumor Research (IMT), BMFZ, Hans-Meerwein-Str. 2, Marburg35043, Germany.ORCID 0000-0003-1344-9117

Funding

German Research Council (DFG) 260989694 and 324652314 (G.B.)German Research Council (DFG) BA2292/1 and BA2292/4 (U.-M.B.)German Research Council (DFG) TRR81 A03 (U.-M.B.) and Z04 (W.D., P.K.)Jos?? Carreras Leuk??mie-Stiftung DJCLS 05 R/2020 (U.-M.B.)
6 · The paper itself

Abstract

A substantial body of research implicates PRMTs in the pathogenesis of human diseases, primarily as oncoproteins or tumor suppressors in cancer. Starting from structure-based in silico screening of small-molecule databases, we predicted, synthesized, and assayed compounds aimed at specifically inhibiting selected PRMT family members. Unexpectedly, among several PRMT-inhibitory molecules we identified TR-07, a compound that selectively enhances the catalytic activity of PRMT1 in vitro. SAR analyses led to the design and synthesis of derivatives with increased potency in activating PRMT1 compared to TR-07 but at the cost of selectivity. TR-07 and its derivatives bind to the αY helix near the catalytic core of PRMT1. Treatment of pancreatic tumor cells with these PRMT1 activators enhanced global ADMA levels and augmented PRMT1's apoptotic function in cell culture and mouse models. Our results establish TR-07 as the first selective, cell-active PRMT1 activator and underscore the therapeutic promise of this novel class of modulators.

Indexed as

Antineoplastic AgentsApoptosisEnzyme ActivatorsPancreatic NeoplasmsProtein-Arginine N-MethyltransferasesRepressor ProteinsSmall Molecule LibrariesAnimalsCell Line, TumorDrug DiscoveryHumansMiceStructure-Activity RelationshipAntineoplastic AgentsEnzyme ActivatorsPRMT1 protein, humanProtein-Arginine N-MethyltransferasesRepressor ProteinsSmall Molecule Libraries

Identifiers

PMID42720487
PMCPMC13576449

What OpenQuestion holds

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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.