Article
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors.
Molecular pharmacology - 1 Jul 2005
Balzarini Jan, Auwerx Joeri, Rodríguez-Barrios Fátima, Chedad Allel, Farkas Viktor, Ceccherini-Silberstein Francesca, García-Aparicio Carlos, Velázquez Sonsoles, De Clercq Erik, Perno Carlo-Federico, Camarasa María-José, Gago Federico
Abstract excerpt
The highly conserved Asn136 is in close proximity to the nonnucleoside reverse transcriptase (RT) inhibitor (NNRTI)-specific lipophilic pocket of human immunodeficiency virus type 1 (HIV-1) RT. Site-directed mutagenesis has revealed that the catalytic activity of HIV-1 RT mutated at position Asn136 is heavily compromised. Only 0.07 to 2.1% of wild-type activity is retained, depending on the nature of the amino...
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