Evidence map›Paper›PMID 32944138›Full record

ArticleACS medicinal chemistry letters2020

Bridgehead Modifications of Englerin A Reduce TRPC4 Activity and Intravenous Toxicity but not Cell Growth Inhibition.

Zhenhua Wu, Jean-Simon Suppo, Sarka Tumova, Jonathan Strope, Fernando Bravo, Melody Moy, Ethan S Weinstein, Cody J Peer, William D Figg, William J Chain and 3 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2020. 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
0.1field-weighted citation impact, top 47% 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

1 citing paper in PubMed, 3 citations in OpenAlex.

  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

13 authors at 5 institutions in 3 countries.

Zhenhua WuDepartment of Chemistry & Biochemistry, University of Delaware, 163 The Green, Newark, Delaware 19716, United States.
Jean-Simon SuppoInstitute of Chemical Research of Catalonia (ICIQ), 43007 Tarragona, Spain.
Sarka TumovaSchool of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
Jonathan StropeGenitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20892, United States.
Fernando BravoInstitute of Chemical Research of Catalonia (ICIQ), 43007 Tarragona, Spain.
Melody MoyDepartment of Chemistry & Biochemistry, University of Delaware, 163 The Green, Newark, Delaware 19716, United States.
Ethan S WeinsteinDepartment of Chemistry & Biochemistry, University of Delaware, 163 The Green, Newark, Delaware 19716, United States.
Cody J PeerGenitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20892, United States.
William D FiggGenitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, Bethesda, Maryland 20892, United States.
William J ChainDepartment of Chemistry & Biochemistry, University of Delaware, 163 The Green, Newark, Delaware 19716, United States.
Antonio M EchavarrenInstitute of Chemical Research of Catalonia (ICIQ), 43007 Tarragona, Spain.
David J BeechSchool of Medicine, University of Leeds, Leeds LS2 9JT, U.K.
John A BeutlerMolecular Targets Program, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, United States.
University of Delaware · USInstitut Català d'Investigació Química · ESNational Cancer Institute · USUniversity of Leeds · GBTarget (United States) · US

Funding

This renovation project will create over 1455 sq. ft. of state- of-the-art reseaP20GM104316 · NIGMS · UNIVERSITY OF DELAWARE · PI SCHMITZ, KARL ROBERT · 2014 to 2024
$26.8M
Drug Development for Prostate Cancer and other Metastatic ProcessesZIABC010547 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI FIGG, WILLIAM DOUGLAS · 2009 to 2025
$10.2M
Development of Natural Product Leads as Anticancer TherapeuticsZIABC011470 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BEUTLER, JOHN · 2012 to 2025
$7.8M
Pilot Research Subproject ProgramP30GM110758 · NIGMS · UNIVERSITY OF DELAWARE · PI PATEL, SANDEEP · 2014 to 2018
$5.8M
Carbonyls to Cancer TherapeuticsR01CA163287 · NCI · UNIVERSITY OF HAWAII AT MANOA · PI CHAIN, WILLIAM JOHN · 2013 to 2016
$1.1M
Q-Exactive Orbitrap LC-MC/MS SystemS10OD016267 · OD · UNIVERSITY OF DELAWARE · PI JOHNSTON, MURRAY V · 2013 to 2013
$573k
High Performance Digital NMR SpectrometerS10RR026962 · NCRR · UNIVERSITY OF DELAWARE · PI FOX, JOSEPH M · 2010 to 2010
$500k
Intramural NIH HHS ZIA BC010547Intramural NIH HHS ZIA BC011470Medical Research Council MC_PC_17165NCI NIH HHS R01 CA163287NCRR NIH HHS S10 RR026962NIGMS NIH HHS P20 GM104316NIGMS NIH HHS P30 GM110758NIH HHS S10 OD016267
6 · The paper itself

Abstract

Modifications at the bridgehead position of englerin A were made to explore the effects of variation at this site on the molecule for biological activity, as judged by the NCI 60 screen, in which englerin A is highly potent and selective for renal cancer cells. Replacement of the isopropyl group by other, larger substituents yielded compounds which displayed excellent selectivity and potency comparable to the natural product. Selected compounds were also evaluated for their effect on the ion channel TRPC4 as well as for intravenous toxicity in mice, and these had lower potency in both assays compared to englerin A.

Identifiers

PMID32944138
PMCPMC7488277
OpenAlexW3047270572

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.