The Heat shock proteins (Hsps) are nowadays considered the most important cell chaperones, which result overexpressed in response to a number of cell stress stimuli.In tumor cells, when Hsp60 accumulates in the cytosol, without mitochondrial release, it exerts an anti-apoptotic effect, by inhibiting pro-caspase-3 (pC3) activation. In this context, our study aims to elucidate the structural details of the interaction between Hsp60 and pC3 and to design novel antagonists able to specifically block this interaction. The analysis of virtual screening results highlights the 4-(3-chloro-4-fluorophenylamino)- 6-[(1H-imidazol-4-yl-methyl)-3-carbonitrile-quinolines of type 1 and the N-{5-[1H-imidazol-4-yl-methyl)-amino]-benzo[b]thiophen-3-yl}-benzamides of type 2 as interesting series for the inhibition of Hsp60 ATP-binding site.

Martorana, A., Palumbo Piccionello, A., Pace, A., Cappello, F., Mingoia, F., Almerico, A.M., et al. (2012). NOVEL ANTAGONISTS FOR AN Hsp60-BASED ANTICANCER CHAPERONOTHERAPY. In 6° Meeeting Nuove Prospettive in Chimica Farmaceutica (pp.85).

NOVEL ANTAGONISTS FOR AN Hsp60-BASED ANTICANCER CHAPERONOTHERAPY

MARTORANA, Annamaria;PALUMBO PICCIONELLO, Antonio;PACE, Andrea;CAPPELLO, Francesco;ALMERICO, Anna Maria;LAURIA, Antonino
2012-01-01

Abstract

The Heat shock proteins (Hsps) are nowadays considered the most important cell chaperones, which result overexpressed in response to a number of cell stress stimuli.In tumor cells, when Hsp60 accumulates in the cytosol, without mitochondrial release, it exerts an anti-apoptotic effect, by inhibiting pro-caspase-3 (pC3) activation. In this context, our study aims to elucidate the structural details of the interaction between Hsp60 and pC3 and to design novel antagonists able to specifically block this interaction. The analysis of virtual screening results highlights the 4-(3-chloro-4-fluorophenylamino)- 6-[(1H-imidazol-4-yl-methyl)-3-carbonitrile-quinolines of type 1 and the N-{5-[1H-imidazol-4-yl-methyl)-amino]-benzo[b]thiophen-3-yl}-benzamides of type 2 as interesting series for the inhibition of Hsp60 ATP-binding site.
Settore CHIM/08 - Chimica Farmaceutica
Settore CHIM/06 - Chimica Organica
Settore BIO/16 - Anatomia Umana
15-apr-2012
6° Meeeting Nuove Prospettive in Chimica Farmaceutica
Riccione
15-17-Aprile-2012
2012
1
Martorana, A., Palumbo Piccionello, A., Pace, A., Cappello, F., Mingoia, F., Almerico, A.M., et al. (2012). NOVEL ANTAGONISTS FOR AN Hsp60-BASED ANTICANCER CHAPERONOTHERAPY. In 6° Meeeting Nuove Prospettive in Chimica Farmaceutica (pp.85).
Proceedings (atti dei congressi)
Martorana, A; Palumbo Piccionello, A; Pace, A; Cappello, F; Mingoia, F; Almerico, AM; Lauria, A
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/64280
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