Evidence map›Paper›PMID 37631011›Full record

ArticlePharmaceuticals (Basel, Switzerland)2023

New Scaffolds of Proteasome Inhibitors: Boosting Anticancer Potential by Exploiting the Synergy of In Silico and In Vitro Methodologies.

Romina A Guedes, Jorge H Grilo, Andreia N Carvalho, Pedro M P Fernandes, Ana S Ressurreição, Vanessa Brito, Adriana O Santos, Samuel Silvestre, Eleonora Gallerani, Maria João Gama and 3 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed, 4 citations in OpenAlex.

  1. Article
  2. Article
  3. 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

13 authors at 3 institutions in 2 countries.

Romina A GuedesResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.ORCID 0000-0002-4397-7968
Jorge H GriloResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.
Andreia N CarvalhoResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.ORCID 0000-0001-9605-5054
Pedro M P FernandesResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.ORCID 0000-0002-2202-4383
Ana S RessurreiçãoResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.
Vanessa BritoHealth Sciences Research Centre (CICS-UBI), University of Beira Interior, 6200-506 Covilhã, Portugal.ORCID 0000-0002-8030-9379
Adriana O SantosHealth Sciences Research Centre (CICS-UBI), University of Beira Interior, 6200-506 Covilhã, Portugal.ORCID 0000-0002-1224-9191
Samuel SilvestreHealth Sciences Research Centre (CICS-UBI), University of Beira Interior, 6200-506 Covilhã, Portugal.ORCID 0000-0003-4297-5108
Eleonora GalleraniDepartment of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, 44121 Ferrara, Italy.
Maria João GamaResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.ORCID 0000-0002-4943-0349
Riccardo GavioliDepartment of Chemical, Pharmaceutical and Agricultural Sciences, University of Ferrara, 44121 Ferrara, Italy.ORCID 0000-0002-7805-4290
Jorge A R SalvadorCenter for Innovative Biomedicine and Biotechnology (CIBB), Center for Neuroscience and Cell Biology (CNC), University of Coimbra, 3004-504 Coimbra, Portugal.ORCID 0000-0003-0779-6083
Rita C GuedesResearch Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, University of Lisbon, 1649-003 Lisboa, Portugal.ORCID 0000-0002-5790-9181
University of Lisbon · PTUniversity of Beira Interior · PTUniversity of Ferrara · IT

Funding

European Commission Centro 2020 Regional Operational Programme under the projects CEN-TRO-01-0247-FEDER-003269 (Drugs2CAD) and CENTRO-01-0145-FEDER-000012 (HealthyAg-ing2020)European Commission LISBOA-01-0145-FEDER-016405 (SAICTPAC/0019/2015)European Union COMPETE 2020-Operational Programme for Competitiveness and InternationalizationFundação para a Ciência e Tecnologia PTDC/QEQ-MED/7042/2014, UID/DTP/04138/2019, SFRH/BD/104441/2014,
6 · The paper itself

Abstract

Cancer is a complex multifactorial disease whose pathophysiology involves multiple metabolic pathways, including the ubiquitin-proteasome system, for which several proteasome inhibitors have already been approved for clinical use. However, the resistance to existing therapies and the occurrence of severe adverse effects is still a concern. The purpose of this study was the discovery of novel scaffolds of proteasome inhibitors with anticancer activity, aiming to overcome the limitations of the existing proteasome inhibitors. Thus, a structure-based virtual screening protocol was developed using the structure of the human 20S proteasome, and 246 compounds from virtual databases were selected for in vitro evaluation, namely proteasome inhibition assays and cell viability assays. Compound

Indexed as

cancerleukemialymphomamolecular dockingmultiple myelomaproteasomeproteasome inhibitorsubiquitin–proteasome systemvirtual screening

Identifiers

PMID37631011
PMCPMC10458307
OpenAlexW4385490860

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.