Evidence map›Paper›PMID 25542669›Full record

ArticleNuclear medicine and biology2015

(125)I-Labelled 2-Iodoestrone-3-sulfate: synthesis, characterization and OATP mediated transport studies in hormone dependent and independent breast cancer cells.

Nilasha Banerjee, T Robert Wu, Jason Chio, Ryan Kelly, Karin A Stephenson, John Forbes, Christine Allen, John F Valliant, Reina Bendayan

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Nuclear medicine and biology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.3field-weighted citation impact, top 39% 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

2 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
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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

9 authors at 2 institutions in 1 country.

Nilasha BanerjeeDepartment of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada.
T Robert WuCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada.
Jason ChioCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada.
Ryan KellyCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada.
Karin A StephensonCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada.
John ForbesCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada.
Christine AllenDepartment of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada.
John F ValliantCentre for Probe Development and Commercialization (CPDC), McMaster University, Hamilton, Ontario, Canada; Department of Chemistry and Chemical Biology, McMaster University, Hamilton, Ontario, Canada. Electronic address: valliant@mcmaster.ca.
Reina BendayanDepartment of Pharmaceutical Sciences, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada. Electronic address: r.bendayan@utoronto.ca.
Centre for Probe Development and Commercialization · CAUniversity of Toronto · CA

Funding

CIHR 87432-1
6 · The paper itself

Abstract

introductionOrganic Anion Transporting Polypeptides (OATP) are a family of membrane associated transporters that facilitate estrone-3-sulphate (E3S) uptake by hormone dependent, post-menopausal breast cancers. We have established E3S as a potential ligand for targeting hormone dependent breast cancer cells, and in this study sought to prepare and investigate radioiodinated E3S as a tool to study the OATP system.

methods2- and 4-Iodoestrone-3-sulfates were prepared from estrone via aromatic iodination followed by a rapid and high yielding sulfation procedure. The resulting isomers were separated by preparative HPLC and verified by (1)H NMR and analytical HPLC. Transport studies of 2- and 4-[(125)I]-E3S were conducted in hormone dependent (i.e. MCF-7) and hormone independent (i.e. MDA-MB-231) breast cancer cells in the presence or absence of the specific transport inhibitor, bromosulfophthalein (BSP). Cellular localization of OATP1A2, OATP2B1, OATP3A1 and OATP4A1 were determined by immunofluorescence analysis using anti-Na(+)/K(+) ATPase-α (1:100 dilution) and DAPI as plasma membrane and nuclear markers, respectively.

resultsSignificantly (p<0.01) higher total accumulation of 2-[(125)I]-E3S was observed in hormone dependent MCF-7 as compared to hormone independent MDA-MB-231 breast cancer cells. In contrast 4-[(125)I]-E3S did not show cellular accumulation in either case. The efficiency of 2-[(125)I]-E3S transport (expressed as a ratio of Vmax/Km) was 2.4 times greater in the MCF-7 as compared to the MDA-MB-231 breast cancer cells. OATP1A2, OATP3A1 and OATP4A1 expression was localized in plasma membranes of MCF-7 and MDA-MB-231 cells confirming the functional role of these transporters in radioiodinated E3S cellular uptake.

conclusionAn efficient method for the preparation of 2- and 4-[(125)I]-E3S was developed and where the former demonstrated potential as an in vitro probe for the OATP system. The new E3S probe can be used to study the OATP system and as a platform to create radiopharmaceuticals for imaging breast cancer.

Indexed as

Breast NeoplasmsCell Line, TumorChemistry Techniques, SyntheticEstroneHormonesHumansIodine RadioisotopesKineticsOrganic Anion TransportersPositron-Emission TomographyProtein IsoformsProtein TransportTomography, Emission-Computed, Single-PhotonEstroneestrone sulfateHormonesIodine RadioisotopesOrganic Anion TransportersProtein IsoformsBreast cancerEstrone-3-sulfateIodine-125Organic anion transporting polypeptide

Identifiers

PMID25542669
PMCPMC5673477
OpenAlexW2043247555

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.