Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity (319 views)
Arkivoc (ISSN: 1424-6376), 2006; 6(VIII): 24-37.
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Paper type: Journal Article,
Impact factor: 0.8, 5-year impact factor: 1.221
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33744470562&partnerID=40&md5=736f517cf4e92d098c00f595b4211328
Keywords: Acetylation, Chromatin Remodelling, Gcn5, Yeast,
Affiliations:
*** 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
References:
Not available.
Arkivoc (ISSN: 1424-6376), 2006; 6(VIII): 24-37.
Export to BibTeX Export to EndNote
Paper type: Journal Article,
Impact factor: 0.8, 5-year impact factor: 1.221
Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-33744470562&partnerID=40&md5=736f517cf4e92d098c00f595b4211328
Keywords: Acetylation, Chromatin Remodelling, Gcn5, Yeast,
Affiliations:
*** 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
References:
Not available.
Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity
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.
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.
Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity
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Identification of small molecules inhibitors of GCN5 histone acetyltransferase activity
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View Export to BibTeX Export to EndNote
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View Export to BibTeX Export to EndNote
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Oncotarget (ISSN: 1949-2553electronic, 1949-2553linking), 2018 May 22; 9(39): 25630-25646.
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View Export to BibTeX Export to EndNote
Magrì A, Tabbì G, Giuffrida A, Pappalardo G, Satriano C, Naletova I, Nicoletti VG, Attanasio F
* Influence of the N-terminus acetylation of Semax, a synthetic analog of ACTH(4-10), on copper(II) and zinc(II) coordination and biological properties (289 views)
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Impact Factor: 3.348
View Export to BibTeX Export to EndNote
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Impact Factor: 4.881
View Export to BibTeX Export to EndNote
Pellerito O, Prinzivalli C, Foresti E, Sabatino P, Abbate M, Casella G, Fiore T, Scopelliti M, Pellerito C, Giuliano M, Grasso G, Pellerito L
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Impact Factor: 3.274
View Export to BibTeX Export to EndNote
Poletto M, Vascotto C, Scognamiglio PL, Lirussi L, Marasco D, Tell G
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Impact Factor: 4.779
View Export to BibTeX Export to EndNote
Lirussi L, Antoniali G, Vascotto C, D'Ambrosio C, Poletto M, Romanello M, Marasco D, Leone M, Quadrifoglio F, Bhakat KK, Scaloni A, Tell G
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Mol Biol Cell (ISSN: 1059-1524), 2012 Oct 15; 23(20): 4079-4096.
Impact Factor: 4.803
View Export to BibTeX Export to EndNote
Poletto M, Di Loreto C, Marasco D, Poletto E, Puglisi F, Damante G, Tell G
* Acetylation on critical lysine residues of Apurinic/apyrimidinic endonuclease 1 (APE1) in triple negative breast cancers (716 views)
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Impact Factor: 2.406
View Export to BibTeX Export to EndNote
Calabrese V, Cornelius C, Cuzzocrea S, Iavicoli I, Rizzarelli E, Calabrese EJ
* Hormesis, cellular stress response and vitagenes as critical determinants in aging and longevity (1138 views)
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Impact Factor: 9.97
View Export to BibTeX Export to EndNote
Milite C, Castellano S, Benedetti R, Tosco A, Ciliberti C, Vicidomini C, Boully L, Franci G, Altucci L, Mai A, Sbardella G
* Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs) (452 views)
Bioorg Med Chem (ISSN: 0968-0896, 1464-3391, 1464-3391electronic), 2011 Jun 15; 19(12): 3690-3701.
Impact Factor: 2.921
View Export to BibTeX Export to EndNote
Fantini D, Vascotto C, Marasco D, D'Ambrosio C, Romanello M, Vitagliano L, Pedone C, Poletto M, Cesaratto L, Quadrifoglio F, Scaloni A, Radicella JP, Tell G
* Critical lysine residues within the overlooked N-terminal domain of human APE1 regulate its biological functions (543 views)
Nucleic Acids Res (ISSN: 1362-4962, 0305-1048, 1362-4962electronic), 2010 Dec; 38(22): 8239-8256.
Impact Factor: 7.836
View Export to BibTeX Export to EndNote
Canettieri G, Di Marcotullio L, Greco A, Coni S, Antonucci L, Infante P, Pietrosanti L, De Smaele E, Ferretti E, Miele E, Pelloni M, De Simone G, Pedone E, Gallinari P, Giorgi A, Steinkuhler C, Vitagliano L, Pedone C, Schinin ME, Screpanti I, Gulino A
* Histone deacetylase and Cullin3-REN(KCTD11) ubiquitin ligase interplay regulates Hedgehog signalling through Gli acetylation (809 views)
Nature Cell Biol Nature Cell Biology (ISSN: 1476-4679, 1465-7392), 2010 Feb; 12(2): 132-142.
Impact Factor: 19.407
View Export to BibTeX Export to EndNote
Chiechio S, Zammataro M, Morales ME, Busceti CL, Drago F, Th Gereau RW, Copani A, Nicoletti F
* Epigenetic modulation of mGlu2 receptors by histone deacetylase inhibitors in the treatment of inflammatory pain (826 views)
Mol Pharmacol (ISSN: 0026-895x), 2009; 75(5): 1014-1020.
Impact Factor: 4.531
View Export to BibTeX Export to EndNote
Sbardella G, Castellano S, Vicidomini C, Rotili D, Nebbioso A, Miceli M, Altucci L, Mai A
* Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases (417 views)
Bioorganic & Medicinal Chemistry Letters (ISSN: 0960-894x), 2008 May 1; 18(9): 2788-2792.
Impact Factor: 2.531
View Export to BibTeX Export to EndNote
Mai A, Rotili D, Tarantino D, Ornaghi P, Tosi F, Vicidomini C, Sbardella G, Nebbioso A, Miceli M, Altucci L, Filetici P
* Small-molecule inhibitors of histone acetyltransferase activity: Identification and biological properties (838 views)
J Med Chem (ISSN: 0022-2623, 1520-4804, 0022-2623print), 2006 Nov 16; 49(23): 6897-6907.
Impact Factor: 5.115
View Export to BibTeX Export to EndNote
Brown DR, Guantieri V, Grasso G, Impellizzeri G, Pappalardo G, Rizzarelli E
* Copper(II) complexes of peptide fragments of the prion protein. Conformation changes induced by copper(II) and the binding motif in C-terminal protein region (661 views)
J Chem Res (ISSN: 0162-0134, 1873-3344, 0162-0134print), 2004 Jan; 98(1): 133-143.
Impact Factor: 2.225
View Export to BibTeX Export to EndNote
17 Records (17 excluding Abstracts).
Total impact factor: 94.601 (94.601 excluding Abstracts).
Total 5 year impact factor: 98.127 (98.127 excluding Abstracts).
Total impact factor: 94.601 (94.601 excluding Abstracts).
Total 5 year impact factor: 98.127 (98.127 excluding Abstracts).
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