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

Humans Lysine Acetyltransferases / metabolism Carcinoma, Non-Small-Cell Lung / drug therapy Lung Neoplasms Histones / metabolism Leukemia, Myeloid, Acute Acetylation Histone Acetyltransferases / metabolism

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
25 05 2023
Historique:
medline: 26 5 2023
pubmed: 8 5 2023
entrez: 8 5 2023
Statut: ppublish

Résumé

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

Identifiants

DOI: 10.1021/acs.jmedchem.2c01937 PMID: 37155735 PMC: PMC10226132
pubmed: 37155735
doi: 10.1021/acs.jmedchem.2c01937
pmc: PMC10226132
doi:

Substances chimiques

Lysine Acetyltransferases EC 2.3.1.32
Histones 0
Histone Acetyltransferases EC 2.3.1.48
KAT8 protein, human EC 2.3.1.48

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

6591-6616

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Auteurs

Francesco Fiorentino (F)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
ORCID: 0000-0003-3550-1860

Sara Sementilli (S)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.

Martina Menna (M)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.

Federica Turrisi (F)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.

Stefano Tomassi (S)

Department of Pharmacy, University of Naples "Federico II", via Domenico Montesano 49, Naples 80131, Italy.
ORCID: 0000-0003-3152-4467

Francesca Romana Pellegrini (FR)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.

Angela Iuzzolino (A)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.

Francesca D'Acunzo (F)

Institute 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 Feoli (A)

Department of Pharmacy, University of Salerno, via Giovanni Paolo II 132, Fisciano (SA) 84084, Italy.
ORCID: 0000-0002-8960-7858

Hannah Wapenaar (H)

Department of Chemical and Pharmaceutical Biology, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands.

Sophie Taraglio (S)

Department of Biochemical Sciences, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.

Caterina Fraschetti (C)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
ORCID: 0000-0002-5095-5388

Donatella Del Bufalo (D)

Preclinical Models and New Therapeutic Agents Unit, IRCCS-Regina Elena National Cancer Institute, Via Elio Chianesi 53, Rome 00144, Italy.

Gianluca Sbardella (G)

Department of Pharmacy, University of Salerno, via Giovanni Paolo II 132, Fisciano (SA) 84084, Italy.
ORCID: 0000-0003-0748-1145

Frank J Dekker (FJ)

Department of Chemical and Pharmaceutical Biology, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands.
ORCID: 0000-0001-7217-9300

Alessandro Paiardini (A)

Department of Biochemical Sciences, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.

Daniela Trisciuoglio (D)

Institute of Molecular Biology and Pathology, National Research Council (CNR), Via degli Apuli 4, Rome 00185, Italy.

Antonello Mai (A)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
Pasteur Institute, Cenci-Bolognetti Foundation, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
ORCID: 0000-0001-9176-2382

Dante Rotili (D)

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, Rome 00185, Italy.
ORCID: 0000-0002-8428-8763

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Acyltransferases › Acetyltransferases › Lysine acetyltransferases › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Maladies de l'appareil respiratoire › Tumeurs de l'appareil respiratoire › Tumeurs du poumon › Tumeurs des bronches › Carcinome bronchogénique › Carcinome pulmonaire non à petites cellules › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Maladies de l'appareil respiratoire › Tumeurs de l'appareil respiratoire › Tumeurs du poumon › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Nucléoprotéines › Histone › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Tumeurs › Tumeurs par type histologique › Leucémies › Leucémie myéloïde › Leucémie aigüe myéloïde › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Métabolisme › Acylation › Acétylation › First-in-Class Selective Inhibitors of the...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Acyltransferases › Acetyltransferases › Lysine acetyltransferases › Histone acetyltransferases › First-in-Class Selective Inhibitors of the...