Evidence map›Paper›PMID 31561530›Full record

ArticleMolecules (Basel, Switzerland)2019

Cyclic Peptides Acting as Allosteric Inhibitors of Human Thymidylate Synthase and Cancer Cell Growth.

Salvatore Pacifico, Matteo Santucci, Rosaria Luciani, Puneet Saxena, Pasquale Linciano, Glauco Ponterini, Angela Lauriola, Domenico D'Arca, Gaetano Marverti, Remo Guerrini and 1 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. 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
0.2field-weighted citation impact, top 47% 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, 5 citations in OpenAlex.

  1. Article
  2. 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

11 authors at 2 institutions in 1 country.

Salvatore PacificoDepartment of Chemical and Pharmaceutical Sciences, University of Ferrara, via Fossato di Mortara 17-19, 44100 Ferrara, Italy. salvatore.pacifico@unife.it.ORCID 0000-0002-3377-5107
Matteo SantucciDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. matteo.santucci86@gmail.com.
Rosaria LucianiDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. rosaria.luciani@libero.it.
Puneet SaxenaDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. puneet_saxena07@yahoo.com.
Pasquale LincianoDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. pasquale.linciano@unimore.it.
Glauco PonteriniDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. glauco.ponterini@unimore.it.ORCID 0000-0002-2115-0775
Angela LauriolaDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. angela.lauriola@unimore.it.
Domenico D'ArcaDepartment of Biomedical Sciences, Metabolic and Neural Sciences, University of Modena and Reggio Emilia, via Campi 287, 41125 Modena, Italy. domenico.darca@unimore.it.ORCID 0000-0002-7240-6005
Gaetano MarvertiDepartment of Biomedical Sciences, Metabolic and Neural Sciences, University of Modena and Reggio Emilia, via Campi 287, 41125 Modena, Italy. gaetano.marverti@unimore.it.ORCID 0000-0002-9074-0795
Remo GuerriniDepartment of Chemical and Pharmaceutical Sciences, University of Ferrara, via Fossato di Mortara 17-19, 44100 Ferrara, Italy. remo.guerrini@unife.it.
Maria Paola CostiDepartment of Life Sciences, University of Modena and Reggio Emilia, via Campi, 103, 41125 Modena, Italy. mariapaola.costi@unimore.it.ORCID 0000-0002-0443-5402
University of Modena and Reggio Emilia · ITUniversity of Ferrara · IT

Funding

Associazione Italiana per la Ricerca sul Cancro IG 10474Associazione Italiana per la Ricerca sul Cancro IG 16977
6 · The paper itself

Abstract

Thymidylate synthase (TS) is a prominent drug target for different cancer types. However, the prolonged use of its classical inhibitors, substrate analogs that bind at the active site, leads to TS overexpression and drug resistance in the clinic. In the effort to identify anti-TS drugs with new modes of action and able to overcome platinum drug resistance in ovarian cancer, octapeptides with a new allosteric inhibition mechanism were identified as cancer cell growth inhibitors that do not cause TS overexpression. To improve the biological properties, 10 cyclic peptides (cPs) were designed from the lead peptides and synthesized. The cPs were screened for the ability to inhibit recombinant human thymidylate synthase (

Indexed as

Allosteric SiteAntineoplastic AgentsBinding SitesCell LineCell Line, TumorDose-Response Relationship, DrugDrug DesignEnzyme ActivationEnzyme InhibitorsHumansModels, MolecularMolecular ConformationMolecular StructurePeptides, CyclicProtein BindingStructure-Activity RelationshipAntineoplastic AgentsEnzyme InhibitorsPeptides, CyclicThymidylate Synthaseallosteric inhibitorsanticancer agentscyclic peptidesenzyme inhibitionovarian cancerthymidylate synthase inhibitors

Identifiers

PMID31561530
PMCPMC6804113
OpenAlexW2977166809

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.