Article
Impact of the enfuvirtide resistance mutation N43D and the associated baseline polymorphism E137K on peptide sensitivity and six-helix bundle structure.
Biochemistry - 24 Jun 2008
Bai Xuefang, Wilson Karen L, Seedorff Jennifer E, Ahrens Douglas, Green Justin, Davison Donna K, Jin Lei, Stanfield-Oakley Sherry A, Mosier Sarah M, Melby Thomas E, Cammack Nick, Wang Zhongmin, Greenberg Michael L, Dwyer John J
Abstract excerpt
Enfuvirtide (ENF), the first human immunodeficiency virus type 1 (HIV-1) fusion inhibitor approved for clinical use, acts by binding to gp41 heptad repeat 1 (HR1) and preventing its interaction with the viral HR2 region. Treatment-emergent resistance to ENF has been mapped to residues within HR1, and these mutations decrease its susceptibility to ENF and may reduce viral fitness and pathogenesis, although the...
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