Evidence map›Paper›PMID 25654690›Full record

ArticleJournal of medicinal chemistry2015

Design, synthesis, and biological evaluation of theranostic vitamin-linker-taxoid conjugates.

Jacob G Vineberg, Tao Wang, Edison S Zuniga, Iwao Ojima

Abstract readEvaluation Study
In one paragraph

Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
–field-weighted citation impact
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

15 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Review
  6. Targeting Strategies for Enhancing Paclitaxel Specificity in Chemotherapy.Frontiers in cell and developmental biology · 2021
    Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Article
  12. Review
  13. Article
  14. Article
  15. 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.

Jacob G VinebergDepartment of Chemistry and ‡Institute of Chemical Biology & Drug Discovery, Stony Brook University , Stony Brook, New York 11794-3400, United States.
Tao Wang
Edison S Zuniga
Iwao Ojima

Funding

Tumor -Targeting Chemotherapeutic AgentsR01CA103314 · NCI · STATE UNIVERSITY NEW YORK STONY BROOK · PI OJIMA, IWAO · 2003 to 2013
$3.1M
NCI NIH HHS CA 103314NCI NIH HHS R01 CA103314
6 · The paper itself

Abstract

Novel tumor-targeting theranostic conjugates 1 and 2, bearing either a fluorine-labeled prosthetic as a potential (18)F-PET radiotracer (1) or a fluorescence probe (2) for internalization studies in vitro, were designed and synthesized. We confirmed efficient internalization of 2 in biotin-receptor positive (BR+) cancer cells via receptor-mediated endocytosis (RME) based on flow cytometry and confocal fluorescence microscopy (CFM) analyses, which exhibited very high specificity to BR+ cancer cells. The potency and cancer-cell selectivity of 1 were evaluated against MX-1, L1210FR and ID8 cancer cells (BR+) as well as L1210 cells and WI38 normal human lung fibroblast cells (biotin-receptor negative: BR-). In particular, we designed and performed an assay in the presence of glutathione ethyl ester (GSH-OEt) wherein only 1 molecules internalized into cells via RME in the first 24 h period exert cytotoxic effect. The observed selectivity of 1 was remarkable, with 2 orders of magnitude difference in IC50 values between BR+ cancer cells and WI38 cells, demonstrating a salient feature of this tumor-targeted drug delivery system.

Indexed as

Drug DesignAnimalsBiotinCells, CulturedDrug Delivery SystemsEndocytosisFibroblastsFlow CytometryHumansLungMiceMicroscopy, ConfocalMicroscopy, FluorescenceMolecular Targeted TherapyNeoplasmsReceptors, Growth FactorBiotinbiotin receptorReceptors, Growth FactorTaxoidsVitamins

Identifiers

PMID25654690
PMCPMC4359053

What OpenQuestion holds

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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.