Article
Kinetic Insights into the Enhanced Antiviral Activity of Islatravir against Doravirine Resistance-Associated Substitution Mutations in HIV-1 Reverse Transcriptase.
Biochemistry - 7 Oct 2025
Zalenski Nikita, Savoie Derek J, Gaur Amit, Patel Neil A, Suo David J, Seay Turner W, Betancourt Daniel, Suo Zucai
Abstract excerpt
Islatravir (ISL, EFdA) is a nucleoside analog that inhibits HIV-1 reverse transcriptase (RT) translocation during viral replication. Its high potency stems from unique structural features: a 4'-ethynyl group that interacts with the hydrophobic pocket (containing A114, Y115, F160, M184, and D185) in HIV-1 RT, hindering translocation, and a 3'-hydroxyl group that mimics natural nucleosides for efficient...
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