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  • Title: 2'-β-Methylselenyl nucleos(t)ide analogs as reverse transcriptase inhibitors against diverse HIV mutants.
    Author: Yoshida Y, Niimi Y, Fushihara D, Katakura H, Fukui R, Murase H, Tomoike F, Hashiya F, Murakami T, Kodama EN, Suzuki T, Yasukawa K, Kimura Y, Abe H.
    Journal: Bioorg Med Chem; 2024 Aug 01; 110():117813. PubMed ID: 38954919.
    Abstract:
    Nucleoside reverse transcriptase inhibitors (NRTIs) have been extensively studied as drugs targeting HIV RT. However, the practice or use of approved NRTIs lacking the 3'-hydroxy group often promotes frequent HIV mutations and generates drug-resistance. Here, we describe a novel NRTI with 2'-β-methylselenyl modification. We found that this modification inhibited the DNA elongation reaction by HIV-1 RT despite having a 3'-hydroxy group. Moreover, the conformation of this nucleoside analog is controlled at C3'-endo, a conformation that resists excision from the elongating DNA by HIV RT. Accordingly, the designed analogs exhibited activity against both wild-type HIV and multidrug-resistant HIV mutants.
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