Sechi, Mario and Bacchi, Alessia and Carcelli, Mauro and Fisicaro, Emilia and Rogolino, Dominga and Gates, Paul and Derudas, Marco and Al-Mawsawi, Laith Q. and Neamati, Nouri (2006) From ligand to complexes: inhibition of HIV-1 Integrase by beta-diketo acid metal complexes. In: SardiniaChem 2006: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive, 5 Giugno 2006, Cagliari, Italia. Conference or Workshop Item.
Recently, a class of compounds bearing a β-diketo acid moiety have emerged as the most promising lead in anti-HIV-1 IN drug discovery. It is believed that the β-diketo acid pharmacophoric motif could be involved in a functional sequestration of one or both divalent metal ions, which are critical cofactors at the enzyme catalytic site. This would subsequently block the transition state of the IN-DNA complex. In this scenario, it is of paramount importance to acquire information about the mode of action of diketo acids, which could then be useful in the design of new compounds as IN inhibitors.
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