Evidence map›Paper›PMID 18392131›Full record

ArticleNeoplasia (New York, N.Y.)2008

A small-molecule furin inhibitor inhibits cancer cell motility and invasiveness.

Julia M Coppola, Mahaveer S Bhojani, Brian D Ross, Alnawaz Rehemtulla

Open access · goldAbstract read
In one paragraph

Article in Neoplasia (New York, N.Y.), 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 59 papers.

0numbers the graph read from it
0cells of the map it votes in
59citing papers in PubMed
2.2field-weighted citation impact, top 11% 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

59 citing papers in PubMed, 99 citations in OpenAlex.

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  11. miR-133a Replacement Attenuates Thoracic Aortic Aneurysm in Mice.Journal of the American Heart Association · 2021
    Article
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  20. Development of Novel DNA-Encoded PCSK9 Monoclonal Antibodies as Lipid-Lowering Therapeutics.Molecular therapy : the journal of the American Society of Gene Therapy · 2019
    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

4 authors at 1 institution in 1 country.

Julia M CoppolaDepartment of Biological Chemistry, University of Michigan Medical School, Ann Arbor, MI 48109, USA.
Mahaveer S Bhojani
Brian D Ross
Alnawaz Rehemtulla
University of Michigan–Ann Arbor · US

Funding

QUANTITATION OF HUMAN BRAIN TUMOR THERAPY RESPONSE BY MRP01CA085878 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ROSS, BRIAN D. · 2001 to 2017
$31.9M
Small Animal Imaging CoreP50CA093990 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ROSS, BRIAN D. · 2002 to 2012
$19.0M
Michigan Small Animal Imaging Resource (MSAIR)R24CA083099 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ROSS, BRIAN D. · 1999 to 2006
$4.2M
NCI NIH HHS P01 CA085878NCI NIH HHS P01CA85878NCI NIH HHS P50 CA093990NCI NIH HHS P50CA093990NCI NIH HHS R24 CA083099NCI NIH HHS R24CA83099
6 · The paper itself

Abstract

Furin, a member the proprotein convertase (PC) family, processes inactive precursor proteins to functional proteins within the Golgi/trans-Golgi network secretory pathway. Furin and other PC family members (furin/PCs) activate proteins vital to proper physiological functioning, including growth factors and hormones, receptors, plasma proteins, and matrix metalloproteases (MMPs). Additionally, the expression and activity of furin/PC are necessary for processing substrates important for cell transformation and tumor progression, metastasis, and angiogenesis. Furin processing of the remodeling protease membrane type-1 matrix metalloproteinase (MT1-MMP) enhances cellular motility and invasiveness, contributing to aggression and metastatic potential cancer cells. Whereas overexpression and activity of furin/PC exacerbate the cancer phenotype, inhibition of its activity decreases or nullifies furin/PC-mediated effects, and thus, inhibition of furin may be a viable route to cancer therapy. Recently, we identified a small-molecule inhibitor of furin, named B3, by high-throughput screening with a K(i) and IC(50) of 12 microM. Here, we show that this cell-permeable, small-molecule compound inhibits furin-mediated cleavage of proMT1-MMP, resulting in decreased MMP-2 activation and cell motility in CHO cells expressing proMT1-MMP. Additionally, this molecule inhibited proMT1-MMP processing, complete MMP-2 maturation, and invasiveness of human fibrosarcoma cells (HT1080).

Indexed as

AnimalsBlotting, WesternCell MovementCells, CulturedCell SurvivalChlorocebus aethiopsCHO CellsCOS CellsCricetinaeCricetulusEnzyme ActivationFibrosarcomaFurinHumansMatrix Metalloproteinase 14Matrix Metalloproteinase 2FurinMatrix Metalloproteinase 14Matrix Metalloproteinase 2MMP14 protein, humanSerine Proteinase Inhibitors

Identifiers

PMID18392131
PMCPMC2288536
OpenAlexW1502782135

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.