A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4' chlorophenyl)thiazol-2-yl)hydrazone. (Articolo in rivista)

Type

• Articolo in rivista (Classe)
• Prodotto della ricerca (Classe)

Label

• A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4' chlorophenyl)thiazol-2-yl)hydrazone. (Articolo in rivista) (literal)

Anno

• 2009-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1021/jm800885d (literal)

Alternative label

• Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A, Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P. (2009)
  A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4' chlorophenyl)thiazol-2-yl)hydrazone.
  in Journal of medicinal chemistry; ACS, American chemical society, Washington, DC (Stati Uniti d'America)
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A, Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P. (literal)

Pagina inizio

• 530 (literal)

Pagina fine

• 536 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

• http://pubs.acs.org/doi/abs/10.1021/jm800885d (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 52 (literal)

Rivista

• Journal of medicinal chemistry (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

• 2 (literal)

Note

• PubMe (literal)
• Scopu (literal)
• Google Scholar (literal)
• ISI Web of Science (WOS) (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• Sapienza Unviersità di Roma, Istituto di Biologia e Patologia Molecolari, CNR (literal)

Titolo

• A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4' chlorophenyl)thiazol-2-yl)hydrazone. (literal)

Abstract

• Acetylation is a key modulator of genome accessibility through decondensation of the chromatin structure. The balance between acetylation and opposite deacetylation is, in fact, a prerequisite for several cell functions and differentiation. To find modulators of the histone acetyltransferase Gcn5p, we performed a phenotypic screening on a set of newly synthesized molecules derived from thiazole in budding yeast Saccharomyces cerevisiae. We selected compounds that induce growth inhibition in yeast strains deleted in genes encoding known histone acetyltransferases. A novel molecule CPTH2, cyclopentylidene-[4-(4?-chlorophenyl)thiazol-2-yl)hydrazone, was selected based on its inhibitory effect on the growth of a gcn5? strain. We demonstrated a specific chemical-genetic interaction between CPTH2 and HAT Gcn5p, indicating that CPTH2 inhibits the Gcn5p dependent functional network. CPTH2 inhibited an in vitro HAT reaction, which is reverted by increasing concentration of histone H3. In vivo, it decreased acetylation of bulk histone H3 at the specific H3-AcK14 site. On the whole, our results demonstrate that CPTH2 is a novel HAT inhibitor modulating Gcn5p network in vitro and in vivo. (literal)

Editore

• ACS, American chemical society (Editore)

Prodotto di

• Institute of molecular biology and pathology (IBPM) (Istituto)
• Struttura e funzione di Acidi nucleici e Cromatina. Epigenetica (SV.P14.009.001) (Modulo)

Autore CNR

• PAOLA BALLARIO (Unità di personale esterno)
• PATRIZIA FILETICI (Unità di personale interno)
• STEFANO VERNARECCI (Persona)

Incoming links:

Prodotto

• Institute of molecular biology and pathology (IBPM) (Istituto)
• Struttura e funzione di Acidi nucleici e Cromatina. Epigenetica (SV.P14.009.001) (Modulo)

Autore CNR di

• PATRIZIA FILETICI (Unità di personale interno)
• STEFANO VERNARECCI (Persona)
• PAOLA BALLARIO (Unità di personale esterno)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• Journal of medicinal chemistry (Rivista)

Editore di

• ACS, American chemical society (Editore)