Evidence map›Paper›PMID 28485901›Full record

ArticleAngewandte Chemie (International ed. in English)2017

Synthesis of a Fluorescent Analogue of Paclitaxel That Selectively Binds Microtubules and Sensitively Detects Efflux by P-Glycoprotein.

Molly M Lee, Zhe Gao, Blake R Peterson

Abstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.

0numbers the graph read from it
0cells of the map it votes in
27citing papers in PubMed
2.3field-weighted citation impact, top 12% 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

27 citing papers in PubMed, 51 citations in OpenAlex.

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  11. Tissue-reactive drugs enable materials-free local depots.Journal of controlled release : official journal of the Controlled Release Society · 2022
    Article
  12. Article
  13. Pacific Blue-Taxoids as Fluorescent Molecular Probes of Microtubules.Methods in molecular biology (Clifton, N.J.) · 2022
    Article
  14. Article
  15. Review
  16. Methoxy and bromo scans onJournal of enzyme inhibition and medicinal chemistry · 2021
    Article
  17. 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

3 authors at 1 institution in 1 country.

Molly M LeeDepartment of Medicinal Chemistry, The University of Kansas, Lawrence, KS, 66045, USA.
Zhe GaoDepartment of Medicinal Chemistry, The University of Kansas, Lawrence, KS, 66045, USA.
Blake R PetersonDepartment of Medicinal Chemistry, The University of Kansas, Lawrence, KS, 66045, USA.ORCID 0000-0001-8251-3579
University of Kansas · US

Funding

Mentoring CoreP20GM103418 · NIGMS · UNIVERSITY OF KANSAS MEDICAL CENTER · PI SUSAN J. BROWN · 2012 to 2026
$63.0M
Understanding the mechanobiology of stem cells in a microengineered 3D cardiac tissue environment with cardiomyopathyP20GM103638 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI HOLMSTROM, ERIK D · 2012 to 2021
$22.1M
U of Kansas/Haskell Indian Nations U.IRACDA ProjectK12GM063651 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI DE GUZMAN, ROBERTO N · 2002 to 2022
$10.0M
TRAINING GRANT IN DYNAMIC ASPECTS OF CHEMICAL BIOLOGYT32GM008545 · NIGMS · UNIVERSITY OF KANSAS LAWRENCE · PI LAMB, AUDREY L · 1994 to 2019
$4.9M
Synthetic Lethal Targeting of Growth Factor ReceptorsR01CA211720 · NCI · UNIVERSITY OF KANSAS LAWRENCE · PI PETERSON, BLAKE · 2017 to 2021
$1.7M
NCI NIH HHS R01 CA211720NIGMS NIH HHS K12 GM063651NIGMS NIH HHS P20 GM103418NIGMS NIH HHS P20 GM103638NIGMS NIH HHS T32 GM008545
6 · The paper itself

Abstract

The anticancer drug paclitaxel (Taxol) exhibits paradoxical and poorly understood effects against slow-growing tumors. To investigate its biological activity, fluorophores such as Oregon Green have been linked to this drug. However, this modification increases its polarity by approximately 1000-fold and reduces the toxicity of Taxol towards cancer cell lines by over 200-fold. To construct more drug-like fluorescent probes suitable for imaging by confocal microscopy and analysis by flow cytometry, we synthesized derivatives of Taxol linked to the drug-like fluorophore Pacific Blue (PB). We found that PB-Gly-Taxol bound the target protein β-tubulin with both high affinity in vitro and high specificity in living cells, exhibited substantial cytotoxicity towards HeLa cells, and was a highly sensitive substrate of the multidrug resistance transporter P-glycoprotein (P-gp).

Indexed as

Antineoplastic Agents, PhytogenicATP Binding Cassette Transporter, Subfamily B, Member 1Binding SitesFlow CytometryFluorescent DyesHeLa CellsHumansMicroscopy, ConfocalMicrotubulesPaclitaxelProtein TransportSubcellular FractionsAntineoplastic Agents, PhytogenicATP Binding Cassette Transporter, Subfamily B, Member 1Fluorescent DyesPaclitaxelantitumor agentsconfocal microscopydrug designfluorescent probespaclitaxel

Identifiers

PMID28485901
PMCPMC5679005
OpenAlexW2613365908

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.