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HIV/AIDS Drug Development

Amino acid Asn136 of HIV-1 RT enables rational design of RT inhibitors

Published in AIDS Weekly, August 22nd, 2005

The amino acid Asn136 of HIV-1 reverse transcriptase enables rational design of RT inhibitors.

According to recent research published in the journal Molecular Pharmacology, "The highly conserved Asn136 is in close proximity to the non-nucleoside 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 acid change at position 136."

"The...

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