Evidence map›Paper›PMID 32962018›Full record

ArticleMolecules (Basel, Switzerland)2020

Cathepsin B-Cleavable Cyclopeptidic Chemotherapeutic Prodrugs.

Viktorija Herceg, Jordan Bouilloux, Karolina Janikowska, Eric Allémann, Norbert Lange

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.6field-weighted citation impact, top 30% 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

5 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
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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

5 authors at 1 institution in 1 country.

Viktorija HercegLaboratory of Pharmaceutical Technology, School of Pharmaceutical Sciences, ISPSO, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneve, Switzerland.
Jordan BouillouxLaboratory of Pharmaceutical Technology, School of Pharmaceutical Sciences, ISPSO, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneve, Switzerland.
Karolina JanikowskaLaboratory of Pharmaceutical Technology, School of Pharmaceutical Sciences, ISPSO, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneve, Switzerland.
Eric AllémannLaboratory of Pharmaceutical Technology, School of Pharmaceutical Sciences, ISPSO, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneve, Switzerland.
Norbert LangeLaboratory of Pharmaceutical Technology, School of Pharmaceutical Sciences, ISPSO, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneve, Switzerland.ORCID 0000-0002-1087-1032
University of Geneva · CH

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Cyclopeptidic chemotherapeutic prodrugs (cPCPs) are macromolecular protease-sensitive doxorubicin (DOX) prodrugs synthesized from a cyclodecapeptidic scaffold, termed Regioselectively Addressable Functionalized Template (RAFT). In order to increase the chemotherapeutic potential of DOX and limit its toxicity, we used a Cathepsin B (Cat B)-sensitive prodrug concept for its targeted release since this enzyme is frequently overexpressed in cancer cells. Copper-free "click" chemistry was used to synthesize cPCPs containing up to four DOX moieties tethered to the upper face of the scaffold through a Cat B-cleavable peptidic linker (GAGRRAAG). On the lower part, PEG 5, 10 and 20 kDa and a fifth peptidyl DOX moiety were grafted in order to improve the solubility, bioavailability and pharmacokinetic profiles of the compound. In vitro results on HT1080 human fibrosarcoma cells showed that cPCPs display a delayed action that consists of a cell cycle arrest in the G2 phase comparable to DOX alone, and increased cell membrane permeability.

Indexed as

Amino Acid SequenceAntibiotics, AntineoplasticCathepsin BCell Line, TumorCell Membrane PermeabilityCell SurvivalClick ChemistryDoxorubicinG2 Phase Cell Cycle CheckpointsHumansPeptides, CyclicPolyethylene GlycolsProdrugsSolubilityAntibiotics, AntineoplasticCathepsin BDoxorubicinPeptides, CyclicPolyethylene GlycolsProdrugscathepsin Bdoxorubicinpoly (ethylene glycol)prodrugRAFT

Identifiers

PMID32962018
PMCPMC7570921
OpenAlexW3087428307

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.