Evidence map›Paper›PMID 39456864›Full record

ArticleInternational journal of molecular sciences2024

Discovery of Novel Thiazole-Based SIRT2 Inhibitors as Anticancer Agents: Molecular Modeling, Chemical Synthesis and Biological Assays.

Francesco Piacente, Giorgia Guccione, Naomi Scarano, Dario Lunaccio, Caterina Miro, Elena Abbotto, Annalisa Salis, Bruno Tasso, Monica Dentice, Santina Bruzzone and 2 more

Abstract read
In one paragraph

Article in International journal of molecular sciences, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
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

12 authors.

Francesco PiacenteDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0000-0001-5470-5987
Giorgia GuccioneDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0009-0007-0175-8912
Naomi ScaranoDepartment of Pharmacy, Section of Medicinal Chemistry, School of Medical and Pharmaceutical Sciences, University of Genoa, Viale Benedetto XV, 3, 16132 Genoa, Italy.ORCID 0000-0002-5121-715X
Dario LunaccioDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0009-0006-5401-8689
Caterina MiroDepartment of Clinical Medicine & Surgery, University of Naples Federico II, Via S. Pansini, 5, 80131 Naples, Italy.ORCID 0000-0002-1008-8443
Elena AbbottoDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0000-0001-7161-6353
Annalisa SalisDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0000-0002-3082-2908
Bruno TassoDepartment of Pharmacy, Section of Medicinal Chemistry, School of Medical and Pharmaceutical Sciences, University of Genoa, Viale Benedetto XV, 3, 16132 Genoa, Italy.ORCID 0000-0002-5636-5645
Monica DenticeDepartment of Clinical Medicine & Surgery, University of Naples Federico II, Via S. Pansini, 5, 80131 Naples, Italy.ORCID 0000-0002-9977-3761
Santina BruzzoneDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0000-0003-2034-3716
Elena CicheroDepartment of Pharmacy, Section of Medicinal Chemistry, School of Medical and Pharmaceutical Sciences, University of Genoa, Viale Benedetto XV, 3, 16132 Genoa, Italy.
Enrico MilloDepartment of Experimental Medicine, Section of Biochemistry, University of Genoa, Viale Benedetto XV, 1, 16132 Genoa, Italy.ORCID 0000-0002-4019-0051

Funding

European Union's Horizon 2020 research and innovation program - Marie Skłodow-ska-Curie 671881University of Genova FRA
6 · The paper itself

Abstract

The search and development of effective sirtuin small molecule inhibitors (SIRTIs) continues to draw great attention due to their wide range of pharmacological applications. Based on SIRTs' involvement in different biological pathways, their ligands were investigated for many diseases, such as cancer, neurodegenerative disorders, diabetes, cardiovascular diseases and autoimmune diseases. The elucidation of a substantial number of SIRT2-ligand complexes is steering the identification of novel and more selective modulators. Among them, SIRT2 in the presence of the SirReal2 analog series was the most studied. On this basis, we recently reported structure-based analyses leading to the discovery of thiazole-based compounds acting as SIRT2 inhibitors (

Indexed as

Antineoplastic AgentsMolecular Docking SimulationSirtuin 2ThiazolesCell Line, TumorDrug DiscoveryHumansLigandsModels, MolecularStructure-Activity RelationshipAntineoplastic AgentsLigandsSIRT2 protein, humanSirtuin 2Thiazolesbiochemical assayscancerdrug designenzymatic assaysinhibitormolecular dockingSIRT2sirtuin

Identifiers

PMID39456864
PMCPMC11508362

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.