A DNA Methyltransferase Modulator Inspired by Peyssonenyne Natural Product Structures. (Articolo in rivista)

Type

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

Label

• A DNA Methyltransferase Modulator Inspired by Peyssonenyne Natural Product Structures. (Articolo in rivista) (literal)

Anno

• 2012-01-01T00:00:00+01:00 (literal)

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

• 10.1002/cmdc.201200366 (literal)

Alternative label

• García-Domínguez P, Weiss M, Lepore I, Alvarez R, Altucci L, Gronemeyer H, de Lera AR. (2012)
  A DNA Methyltransferase Modulator Inspired by Peyssonenyne Natural Product Structures.
  in ChemMedChem (Print)
  (literal)

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

• García-Domínguez P, Weiss M, Lepore I, Alvarez R, Altucci L, Gronemeyer H, de Lera AR. (literal)

Rivista

• ChemMedChem (Rivista)

Note

• PubMe (literal)

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

• Departamento de Química Orgánica, Facultade de Química, Universidade de Vigo, 36310 Vigo (Spain) Department of Cancer Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire (IGBMC)/CNRS/INSERM/ULP, BP 163, 67404 Illkirch Cedex, C.U. de Strasbourg (France) Dipartimento di Patologia Generale, Seconda Università degli Studi di Napoli, Vico L. de Crecchio 7, 80138 Napoli (Italy) CNR-IGB, via P. Castellino, 80100 Napoli (Italy) (literal)

Titolo

• A DNA Methyltransferase Modulator Inspired by Peyssonenyne Natural Product Structures. (literal)

Abstract

• novel epigenetic modulator that displays a DNMT1 inhibition and DNMT3A activation profile was characterized (compound 8). This compound is a derivative of palmitic acid that incorporates the putative reactive functional group (diynone) of the peyssonenyne natural products. Other analogues containing the diynone or an acetoxyenediyne did not show the same biological profile. In U937 human leukemia cells, diynone 8 induced cell differentiation and apoptosis, which correlated with the expression of Fas protein. Very surprisingly, diynone 8 was toxic to normal human fibroblasts (BJ) and mouse embryo fibroblasts (MEF), but not to immortalized human fibroblasts (BJEL); this unique effect was not observed with the classical DNMT inhibitor 5-azacytidine. Therefore, compound 8 interferes in a very specific manner with signaling pathways, the activities of which differ between normal and immortalized cell types. This toxicity is reminiscent of the effects of Dnmt1 ablation on mouse fibroblasts. In fact, some of the genes deregulated by the loss of Dnmt1 are similarly deregulated by 8, but not by the DNMT inhibitor SGI-1027. (literal)

Prodotto di

• Institute of genetics and biophysics \"Adriano Buzzati Traverso\" (IGB) (Istituto)
• Identificazione di regolatori del differenziamento, della motilità e dell'apoptosi delle cellule staminali (SV.P15.008.001) (Modulo)

Autore CNR

• Lucia Altucci (Unità di personale esterno)

Incoming links:

Prodotto

• Institute of genetics and biophysics \"Adriano Buzzati Traverso\" (IGB) (Istituto)
• Identificazione di regolatori del differenziamento, della motilità e dell'apoptosi delle cellule staminali (SV.P15.008.001) (Modulo)

Autore CNR di

• Lucia Altucci (Unità di personale esterno)

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

• ChemMedChem (Rivista)