Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clinical candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo / P. Jones, S. Altamura, R. De Francesco, O.G. Paz, O. Kinzel, G. Mesiti, E. Monteagudo, G. Pescatore, M. Rowley, M. Verdirame, C. Steinkühler. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 51:8(2008), pp. 2350-2353.

A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo

R. De Francesco;
2008

Abstract

Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clinical candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors.
English
cancer; fermentation; taxonomy; therapy; agent; HDAC
Settore BIO/11 - Biologia Molecolare
Articolo
Esperti anonimi
Ricerca di base
Pubblicazione scientifica
2008
51
8
2350
2353
4
Pubblicato
Periodico con rilevanza internazionale
Aderisco
info:eu-repo/semantics/article
A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo / P. Jones, S. Altamura, R. De Francesco, O.G. Paz, O. Kinzel, G. Mesiti, E. Monteagudo, G. Pescatore, M. Rowley, M. Verdirame, C. Steinkühler. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 51:8(2008), pp. 2350-2353.
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Article (author)
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P. Jones, S. Altamura, R. De Francesco, O.G. Paz, O. Kinzel, G. Mesiti, E. Monteagudo, G. Pescatore, M. Rowley, M. Verdirame, C. Steinkühler...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/662292
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