Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity
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Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity (131 visite)

Mai A, Rotili D, Ornaghi P, Tosi F, Vicidomini C, Sardella G, Nebbioso A, Altucci L, Filatici P

Arkivoc (ISSN: 1424-6376), 2006; 6(VIII): 24-37.



Tipo di articolo: Journal Article,

Impact factor: 0.8, Impact factor a 5 anni: 1.221

Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33744470562&partnerID=40&md5=736f517cf4e92d098c00f595b4211328

Parole chiave: Acetylation, Chromatin Remodelling, Gcn5, Yeast,

Affiliazioni:

*** IBB - CNR ***
Istituto Pasteur - Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universit degli Studi di Roma La Sapienza, P. le A. Moro 5, 00185 Roma, Italy
Dipartimento di Genetica e Biologia Molecolare, Universit degli Studi di Roma La Sapienza, P. le A. Moro 5, 00185 Roma, Italy
Dipartimento di Scienze Farmaceutiche, Universit degli Studi di Salerno, via Ponte Don Melillo, 84084 Fisciano (SA), Italy
Dipartimento di Patologia Generale, Seconda Universit degli Studi di Napoli, vico L. De Crecchio 7, 80138 Napoli, Italy
Centro di Oncogenomica AIRC, CEINGE Biotecnologia Avanzata, Napoli, Italy
Istituto di Biologia e Patologia Molecolari CNR, Dip. Genetica e Biologia Molecolare, Universit degli Studi di Roma La Sapienza, P. le A. Moro 5, 00185 Roma, Italy


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Starting from a yeast phenotypic screening performed on 21 chemically different substances we described the discovery of two small molecules as GCN5 inhibitors. The 2-methyl-3-carbethoxyquinoline 9 and its 2-desmethyl analogue 18 were able to significantly reduce the yeast cell growth, thus miming the effect of GCN5 deletion mutant. Tested to evaluate their effect on GCN5-dependent transcription of the HIS3 gene, 9 and 18 showed high inhibitory activity of gene transcription, more evident in activated conditions. Compound 9 was also able to reduce the acetylation levels of H3 and, to a lesser extent, H4 in yeast at 0.6 mM. In human leukemia U937 cells, at 1 mM concentration 9 showed 27% apoptosis induction, while 18 had just a little effect in the same conditions. Further studies on 9 and 18 will be performed to deepen their effects on GCN5-related phenomena.
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