Evidence map›Paper›PMID 37155735›Full record

ArticleJournal of medicinal chemistry2023

First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8.

Francesco Fiorentino, Sara Sementilli, Martina Menna, Federica Turrisi, Stefano Tomassi, Francesca Romana Pellegrini, Angela Iuzzolino, Francesca D'Acunzo, Alessandra Feoli, Hannah Wapenaar and 9 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
3.2field-weighted citation impact, top 8% 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

11 citing papers in PubMed, 21 citations in OpenAlex.

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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

19 authors at 8 institutions in 2 countries.

Francesco FiorentinoDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.ORCID 0000-0003-3550-1860
Sara SementilliInstitute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.
Martina MennaDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
Federica TurrisiInstitute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.
Stefano TomassiDepartment of Pharmacy, University of Naples "Federico II", via Domenico Montesano 49, Naples 80131, Italy.ORCID 0000-0003-3152-4467
Francesca Romana PellegriniInstitute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.
Angela IuzzolinoInstitute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.
Francesca D'AcunzoInstitute of Biological Systems (ISB), Italian National Research Council (CNR), Sezione Meccanismi di Reazione, c/o Department of Chemistry, Sapienza University of Rome, P. le A. Moro 5, Rome 00185, Italy.
Alessandra FeoliDepartment of Pharmacy, University of Salerno, via Giovanni Paolo II 132, Fisciano (SA) 84084, Italy.ORCID 0000-0002-8960-7858
Hannah WapenaarDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands.
Sophie TaraglioDepartment of Biochemical Sciences, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
Caterina FraschettiDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.ORCID 0000-0002-5095-5388
Donatella Del BufaloPreclinical Models and New Therapeutic Agents Unit, IRCCS-Regina Elena National Cancer Institute, Via Elio Chianesi 53, Rome 00144, Italy.
Gianluca SbardellaDepartment of Pharmacy, University of Salerno, via Giovanni Paolo II 132, Fisciano (SA) 84084, Italy.ORCID 0000-0003-0748-1145
Frank J DekkerDepartment of Chemical and Pharmaceutical Biology, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands.ORCID 0000-0001-7217-9300
Alessandro PaiardiniDepartment of Biochemical Sciences, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
Daniela TrisciuoglioInstitute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.
Antonello MaiDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.ORCID 0000-0001-9176-2382
Dante RotiliDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.ORCID 0000-0002-8428-8763
Sapienza University of Rome · ITInstitute of Molecular Biology and Pathology · ITUniversity of Groningen · NLUniversity of Salerno · ITIstituti di Ricovero e Cura a Carattere Scientifico · ITIstituto Pasteur · ITNational Research Council · ITUniversity of Naples Federico II · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

KAT8 is a lysine acetyltransferase primarily catalyzing the acetylation of Lys16 of histone H4 (H4K16). KAT8 dysregulation is linked to the development and metastatization of many cancer types, including non-small cell lung cancer (NSCLC) and acute myeloid leukemia (AML). Few KAT8 inhibitors have been reported so far, none of which displaying selective activity. Based on the KAT3B/KDAC inhibitor C646, we developed a series of

Indexed as

Carcinoma, Non-Small-Cell LungLeukemia, Myeloid, AcuteLung NeoplasmsLysine AcetyltransferasesAcetylationHistone AcetyltransferasesHistonesHumansHistone AcetyltransferasesHistonesKAT8 protein, humanLysine Acetyltransferases

Identifiers

PMID37155735
PMCPMC10226132
OpenAlexW4375954582

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.