Evidence map›Paper›PMID 29859013›Full record

ArticleBritish journal of pharmacology2018

Tonantzitlolone is a nanomolar potency activator of transient receptor potential canonical 1/4/5 channels.

Hussein N Rubaiy, Melanie J Ludlow, Karsten Siems, Katherine Norman, Richard Foster, Dietmar Wolf, John A Beutler, David J Beech

Open access · bronzeAbstract read
In one paragraph

Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
1.5field-weighted citation impact, top 18% of its field
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

16 citing papers in PubMed, 32 citations in OpenAlex.

  1. Article
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  4. Expression of pH-Sensitive TRPC4 in Common Skin Tumors.International journal of molecular sciences · 2023
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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

8 authors at 3 institutions in 3 countries.

Hussein N RubaiySchool of Medicine, University of Leeds, Leeds, UK.ORCID 0000-0002-1489-5576
Melanie J LudlowSchool of Medicine, University of Leeds, Leeds, UK.
Karsten SiemsAnalytiCon Discovery GmbH, Potsdam, Germany.
Katherine NormanSchool of Chemistry, University of Leeds, Leeds, UK.
Richard FosterSchool of Chemistry, University of Leeds, Leeds, UK.
Dietmar WolfAnalytiCon Discovery GmbH, Potsdam, Germany.
John A BeutlerMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, MD, USA.
David J BeechSchool of Medicine, University of Leeds, Leeds, UK.
University of Leeds · GBClimate Analytics · DETarget (United States) · US

Funding

Development of Natural Product Leads as Anticancer TherapeuticsZIABC011470 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BEUTLER, JOHN · 2012 to 2025
$7.8M
Medical Research Council MC_PC_17165The Wellcome TrustWellcome Trust
6 · The paper itself

Abstract

background and purposeThe diterpene ester tonantzitlolone (TZL) is a natural product, which displays cytotoxicity towards certain types of cancer cell such as renal cell carcinoma cells. The effect is similar to that of (-)-englerin A, and so, although it is chemically distinct, we investigated whether TZL also targets transient receptor potential canonical (TRPC) channels of the 1, 4 and 5 type (TRPC1/4/5 channels). EXPERIMENTAL APPROACH: The effects of TZL on renal cell carcinoma A498 cells natively expressing TRPC1 and TRPC4, modified HEK293 cells overexpressing TRPC4, TRPC5, TRPC4-TRPC1 or TRPC5-TRPC1 concatemer, TRPC3 or TRPM2, or CHO cells overexpressing TRPV4 were studied by determining changes in intracellular Ca KEY

resultsTZL induced an elevation of intracellular Ca CONCLUSIONS AND IMPLICATIONS: TZL is a novel potent agonist for TRPC1/4/5 channels, which should be useful for testing the functionality of this type of ion channel and understanding how TRPC1/4/5 agonists achieve selective cytotoxicity against certain types of cancer cell.

Indexed as

AnimalsAntineoplastic AgentsCalciumCell Line, TumorCHO CellsCricetulusDiterpenesHEK293 CellsHumansMacrocyclic CompoundsTRPC Cation ChannelsAntineoplastic AgentsCalciumDiterpenesMacrocyclic CompoundstonantzitloloneTRPC Cation Channels

Identifiers

PMID29859013
PMCPMC6057908
OpenAlexW2806611048

What OpenQuestion holds

Textmetadata
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.