Abstract

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.
Lingua originaleEnglish
Pagine85-
Numero di pagine1
Stato di pubblicazionePublished - 2012

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