CPTH6, a thiazole-derivative, induces histone hypoacetylation and apoptosis in human leukemia cells (Articolo in rivista)

Type

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

Label

• CPTH6, a thiazole-derivative, induces histone hypoacetylation and apoptosis in human leukemia cells (Articolo in rivista) (literal)

Anno

• 2012-01-01T00:00:00+01:00 (literal)

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

• 10.1158/1078-0432.CCR-11-0579 (literal)

Alternative label

• Trisciuoglio Daniela1; Ragazzoni Ylenia1; Pelosi Andrea2; Desideri Marianna1; Carradori Simone4; Gabellini Chiara1,3; Maresca Giovanna7; Nescatelli Riccardo5; Secci Daniela4;Bolasco Adriana 4; Bizzarri Bruna4; Cavaliere Chiara5; D'Agnano Igea7; Filetici Patrizia6; Ricci-Vitiani Lucia8; Rizzo Maria Giulia2; Del Bufalo Donatella1 (2012)
  CPTH6, a thiazole-derivative, induces histone hypoacetylation and apoptosis in human leukemia cells
  in Clinical cancer research (Print)
  (literal)

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

• Trisciuoglio Daniela1; Ragazzoni Ylenia1; Pelosi Andrea2; Desideri Marianna1; Carradori Simone4; Gabellini Chiara1,3; Maresca Giovanna7; Nescatelli Riccardo5; Secci Daniela4;Bolasco Adriana 4; Bizzarri Bruna4; Cavaliere Chiara5; D'Agnano Igea7; Filetici Patrizia6; Ricci-Vitiani Lucia8; Rizzo Maria Giulia2; Del Bufalo Donatella1 (literal)

Pagina inizio

• 475 (literal)

Pagina fine

• 486 (literal)

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

• 18 (literal)

Rivista

• Clinical cancer research (Rivista)

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

• 11 (literal)

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

• 2 (literal)

Note

• ISI Web of Science (WOS) (literal)
• PubMe (literal)

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

• 1Experimental Chemotherapy Laboratory and 2Molecular Oncogenesis Laboratory, Regina Elena National Cancer Institute; Departments of 3Anatomy, Histology, Forensic Medicine, Orthopedics, Section of Histology and Medical Embryology, 4Chemistry and Pharmaceutical Technologies, 5Chemistry and 6Institute of Molecular Biology and Pathology, CNR, \"Sapienza\" University; 7Institute of Cell Biology and Neurobiology-CNR Santa Lucia Foundation-IRCCS; and 8Department of Hematology, Oncology, and Molecular Medicine, Istituto Superiore di Sanità, Rome, Italy. (literal)

Titolo

• CPTH6, a thiazole-derivative, induces histone hypoacetylation and apoptosis in human leukemia cells (literal)

Abstract

• Purpose: We previously identified novel thiazole derivatives able to reduce histone acetylation and histone acetyltransferase (HAT) activity in yeast. Among these compounds, 3-methylcyclopentylidene- [4-(40-chlorophenyl)thiazol-2-yl]hydrazone (CPTH6) has been selected and used throughout this study. Experimental Design: The effect of CPTH6 on histone acetylation, cell viability and differentiation, cellcycle distribution, and apoptosis in a panel of acute myeloid leukemia and solid tumor cell lines has been evaluated. Results: Here, we showed that CPTH6 leads to an inhibition of Gcn5 and pCAF HATactivity. Moreover, it inhibits H3/H4 histones and a-tubulin acetylation of a panel of leukemia cell lines. Concentration- and time-dependent inhibition of cell viability, paralleled by accumulation of cells in the G0/G1 phase and depletion from the S/G2M phases, was observed. The role of mitochondrial pathway on CPTH6-induced apoptosis was shown, being a decrease of mitochondrial membrane potential and the release of cytochrome c, from mitochondria to cytosol, induced by CPTH6. Also the involvement of Bcl-2 and Bcl-xL on CPTH6- induced apoptosis was found after overexpression of the two proteins in leukemia cells. Solid tumor cell lines from several origins were shown to be differently sensitive to CPTH6 treatment in terms of cell viability, and a correlation between the inhibitory efficacy on H3/H4 histones acetylation and cytotoxicity was found. Differentiating effect on leukemia and neuroblastoma cell lines was also induced by CPTH6. Conclusions: These results make CPTH6 a suitable tool for discovery of molecular targets of HAT and, potentially, for the development of new anticancer therapies, which warrants further investigations. (literal)

Prodotto di

• ex ME.P03.007.001 / Meccanismi regolativi del Differenziamento e Oncogenesi (ME.P03.007.002) (Modulo)
• Institute of molecular biology and pathology (IBPM) (Istituto)
• Struttura e funzione di Acidi nucleici e Cromatina. Epigenetica (SV.P14.009.001) (Modulo)

Autore CNR

• PATRIZIA FILETICI (Unità di personale interno)
• IGEA D'AGNANO (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)
• ex ME.P03.007.001 / Meccanismi regolativi del Differenziamento e Oncogenesi (ME.P03.007.002) (Modulo)

Autore CNR di

• PATRIZIA FILETICI (Unità di personale interno)
• IGEA D'AGNANO (Persona)

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

• Clinical cancer research (Rivista)