Article
High potency of indolyl aryl sulfone nonnucleoside inhibitors towards drug-resistant human immunodeficiency virus type 1 reverse transcriptase mutants is due to selective targeting of different mechanistic forms of the enzyme.
Antimicrobial agents and chemotherapy - 1 Nov 2005
Cancio Reynel, Silvestri Romano, Ragno Rino, Artico Marino, De Martino Gabriella, La Regina Giuseppe, Crespan Emmanuele, Zanoli Samantha, Hübscher Ulrich, Spadari Silvio, Maga Giovanni
Abstract excerpt
Indolyl aryl sulfone (IAS) nonnucleoside inhibitors have been shown to potently inhibit the growth of wild-type and drug-resistant human immunodeficiency virus type 1 (HIV-1), but their exact mechanism of action has not been elucidated yet. Here, we describe the mechanism of inhibition of HIV-1 reverse transcriptase (RT) by selected IAS derivatives. Our results showed that, depending on the substitutions...
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