Evidence map›Paper›PMID 22425885›Full record

ArticleInternational journal of pharmaceutics2012

Synthesis and in vitro evaluation of novel lipophilic monophosphorylated gemcitabine derivatives and their nanoparticles.

Dharmika S P Lansakara-P, B Leticia Rodriguez, Zhengrong Cui

Erratum issuedOpen access · greenAbstract readComparative Study
In one paragraph

Article in International journal of pharmaceutics, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
2.2field-weighted citation impact, top 13% 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

18 citing papers in PubMed, 44 citations in OpenAlex.

  1. Article
  2. Review
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  4. Review
  5. Review
  6. Oral 4-(Oncotarget · 2017
    Article
  7. Article
  8. Review
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  17. Article
  18. Gemcitabine-(CJournal of clinical & experimental oncology
    Article
4 · The record

Corrections and comments

  • Erratum issued
5 · Who and what money

Authors and funding

3 authors at 2 institutions in 1 country.

Dharmika S P Lansakara-PThe University of Texas at Austin, College of Pharmacy, Pharmaceutics Division, Austin, TX 78712, United States.
B Leticia Rodriguez
Zhengrong Cui
Austin College · USThe University of Texas at Austin · US

Funding

Overcoming pancreatic tumor resistance to gemcitabineR01CA135274 · NCI · UNIVERSITY OF TEXAS AT AUSTIN · PI CUI, ZHENGRONG · 2008 to 2017
$2.8M
NCI NIH HHS CA135274NCI NIH HHS R01 CA135274
6 · The paper itself

Abstract

Gemcitabine hydrochloride (HCl) is approved for the treatment of a wide spectrum of solid tumors. However, the rapid development of resistance often makes gemcitabine less efficacious. In the present study, we synthesized several novel lipophilic monophosphorylated gemcitabine derivatives, incorporated them into solid lipid nanoparticles, and then evaluated their ability to overcome major known gemcitabine resistance mechanisms by evaluating their in vitro cytotoxicities in cancer cells that are deficient in deoxycytidine kinase (dCK), deficient in human equilibrative nucleoside transporter (hENT1), over-expressing ribonucleotide reductase M1 subunit (RRM1), or over-expressing RRM2. In dCK deficient cells, the monophosphorylated gemcitabine derivatives and their nanoparticles were up to 86-fold more cytotoxic than gemcitabine HCl. The majority of the gemcitabine derivatives and their nanoparticles were more cytotoxic than gemcitabine HCl in cells that over-expressing RRM1 or RRM2, and the gemcitabine derivatives in nanoparticles were also resistant to deamination by deoxycytidine deaminase. The gemcitabine derivatives (in nanoparticles) hold a great potential in overcoming gemcitabine resistance.

Indexed as

NanoparticlesAnimalsAntimetabolites, AntineoplasticCell Line, TumorDeoxycytidineDeoxycytidine KinaseDrug Resistance, NeoplasmDrug Screening Assays, AntitumorEquilibrative Nucleoside Transporter 1GemcitabineGene Expression Regulation, NeoplasticHumansLipidsMiceNeoplasmsRibonucleoside Diphosphate ReductaseAntimetabolites, AntineoplasticDeoxycytidineDeoxycytidine KinaseEquilibrative Nucleoside Transporter 1GemcitabineLipidsRibonucleoside Diphosphate Reductaseribonucleotide reductase M2RRM1 protein, humanSLC29A1 protein, humanTumor Suppressor Proteins

Identifiers

PMID22425885
PMCPMC3335205
OpenAlexW2061869172

What OpenQuestion holds

Textmetadata
LicenceTDM
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.