Evidence map›Paper›PMID 41879799›Full record

ArticleACS chemical biology2026

Selective TRPV2 Antagonists Derived from the Natural Product Piperlongumine Inhibit Cancer Cell Migration and Metastasis.

Hannah Kiely-Collins, Cong Tang, Marta C Marques, Laura Butron, Angela Lamberti, Nicholas Bossons, Fabian Offensperger, Vincenth Brennsteiner, Bárbara Sousa, Luís Carvalho and 5 more

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In one paragraph

Article in ACS chemical biology, 2026. 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
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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

15 authors.

Hannah Kiely-CollinsYusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K.
Cong TangGIMM - Gulbenkian Institute for Molecular Medicine, Avenida Prof. Egas Moniz, Lisboa 1649-028, Portugal.ORCID 0000-0003-1661-6793
Marta C MarquesGIMM - Gulbenkian Institute for Molecular Medicine, Avenida Prof. Egas Moniz, Lisboa 1649-028, Portugal.
Laura ButronInstituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernandez, Avda. Universidad s/n, Elche 03202, Spain.
Angela LambertiInstituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernandez, Avda. Universidad s/n, Elche 03202, Spain.ORCID 0009-0001-9191-0004
Nicholas BossonsChemprecise Lda, Torres Vedras 2560-247, Portugal.
Fabian OffenspergerCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna 1090, Austria.ORCID 0009-0008-4304-2346
Vincenth BrennsteinerCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna 1090, Austria.
Bárbara SousaGIMM - Gulbenkian Institute for Molecular Medicine, Avenida Prof. Egas Moniz, Lisboa 1649-028, Portugal.
Luís CarvalhoYusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K.
Antonio Ferrer-MontielInstituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernandez, Avda. Universidad s/n, Elche 03202, Spain.
Francisco CorzanaDepartamento de Química, Universidad de La Rioja, Instituto de Investigación en Química (IQUR), Logroño 26006, Spain.ORCID 0000-0001-5597-8127
Georg E WinterCeMM Research Center for Molecular Medicine of the Austrian Academy of Sciences, Vienna 1090, Austria.ORCID 0000-0001-6606-1437
Asia Fernandez-CarvajalInstituto de Investigación, Desarrollo e Innovación en Biotecnología Sanitaria de Elche (IDiBE), Universidad Miguel Hernandez, Avda. Universidad s/n, Elche 03202, Spain.
Gonçalo J L BernardesYusuf Hamied Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, U.K.ORCID 0000-0001-6594-8917

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

TRPV2 is the least studied member of the vanilloid TRP subfamily despite its emerging relevance in cancer metastasis, pain, and inflammation. Although several small-molecule TRPV2 modulators have been reported, including the natural products piperlongumine (PL) and cannabidiol, all lack selectivity, complicating the interpretation of phenotypic readouts and functional insights into the role of the channel in health and disease. Here, we report a series of PL-based derivatives rationally designed to maintain TRPV2 antagonism while eliminating covalent off-target activity associated with the electrophilic groups present in PL. Using electrophysiological and calcium fluorescence imaging assays in HEK293T cells and DRG nociceptors, we identified HKC54 as the most potent TRPV2 antagonist to date (IC

Indexed as

Antineoplastic AgentsBiological ProductsCell MovementDioxolanesTRPV Cation ChannelsAnimalsCell Line, TumorHEK293 CellsHumansNeoplasm MetastasisPiperidonesAntineoplastic AgentsBiological ProductsDioxolanesPiperidonespiperlongumineTRPV2 protein, humanTRPV Cation Channels

Identifiers

PMID41879799
PMCPMC13097083

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LicenceCC BY
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Registered trials

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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.