TY - CONF
T1 - NOVEL ANTAGONISTS FOR AN Hsp60-BASED ANTICANCERCHAPERONOTHERAPY
AU - Almerico, Anna Maria
AU - Cappello, Francesco
AU - Lauria, Antonino
AU - Palumbo Piccionello, Antonio
AU - Pace, Andrea
AU - Martorana, Annamaria
PY - 2012
Y1 - 2012
N2 - The Heatshock proteins (Hsps) are nowadays considered the most important cell chaperones,which result overexpressed in response to a number of cell stress stimuli.In tumorcells, when Hsp60 accumulates in the cytosol, without mitochondrial release, it exertsan anti-apoptotic effect, by inhibiting pro-caspase-3 (pC3) activation. In this context, our study aims to elucidate the structural details of the interactionbetween Hsp60 and pC3 and to design novel antagonists able to specifically block thisinteraction. 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 theN-{5-[1H-imidazol-4-yl-methyl)-amino]-benzo[b]thiophen-3-yl}-benzamides of type 2 asinteresting series for the inhibition of Hsp60 ATP-binding site.
AB - The Heatshock proteins (Hsps) are nowadays considered the most important cell chaperones,which result overexpressed in response to a number of cell stress stimuli.In tumorcells, when Hsp60 accumulates in the cytosol, without mitochondrial release, it exertsan anti-apoptotic effect, by inhibiting pro-caspase-3 (pC3) activation. In this context, our study aims to elucidate the structural details of the interactionbetween Hsp60 and pC3 and to design novel antagonists able to specifically block thisinteraction. 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 theN-{5-[1H-imidazol-4-yl-methyl)-amino]-benzo[b]thiophen-3-yl}-benzamides of type 2 asinteresting series for the inhibition of Hsp60 ATP-binding site.
UR - http://hdl.handle.net/10447/64280
M3 - Other
SP - 85-
ER -