Article
Mechanism of interaction of novel indolylarylsulfone derivatives with K103N and Y181I mutant HIV-1 reverse transcriptase in complex with its substrates.
Antiviral chemistry & chemotherapy - 17 Nov 2011
Samuele Alberta, Bisi Sara, Kataropoulou Alexandra, La Regina Giuseppe, Piscitelli Francesco, Gatti Valerio, Silvestri Romano, Maga Giovanni
Abstract excerpt
BACKGROUND: Novel indolylarylsulfones (IASs), designed through rational structure-based molecular modelling and docking approaches, have been recently characterized as effective inhibitors of the wild-type and drug-resistant mutant HIV-1 reverse transcriptase (RT). METHODS: Here, we studied the interaction of selected halo- and nitro-substituted IAS derivatives, with the RT enzyme carrying the single resistance...
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