Sechi, Mario and Carta, Fabrizio and Sannia, Luciano and Dallocchio, Roberto and Dessì, Alessandro and Cosseddu, Alessia and Neamati, Nouri (2008) Design, synthesis, molecular modeling and anti-HIV 1 integrase activity of a series of photoactivable diketo acid-containing inhibitors as affinity probes. In: SardiniaChem 2008: giornata di studio dedicata alla chimica organica delle molecole biologicamente attive, 30 Maggio 2008, Sassari, Italia. Conference or Workshop Item.
Photoaffinity Labelling (PL) is a powerful method in the chemical proteomic approach of protein functions. This method is especially useful for the identification of ligand-binding sites of target proteins and for the investigation of ligand–receptor interactions. The use of affinity-labeled inhibitors to covalently modify the site of interaction and subsequent analysis of the protein have been very effective in providing useful informations about inhibitor binding for a multitude of therapeutic target proteins. Therefore, it could reasonably be applied in drug discovery and development processes. For example, such approach can be used to obtain structural information detailing the association between the enzyme HIV-1 integrase (IN) and inhibitors under development.
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