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- Title
Selection of gp41-mediated HIV-1 cell entry inhibitors from biased combinatorial libraries of non-natural binding elements.
- Authors
Ferrer, M; Kapoor, T M; Strassmaier, T; Weissenhorn, W; Skehel, J J; Oprian, D; Schreiber, S L; Wiley, D C; Harrison, S C
- Abstract
The trimeric, alpha-helical coiled-coil core of the HIV-1 gp41 ectodomain is thought to be part of a transient, receptor-triggered intermediate in the refolding of the envelope glycoprotein into a fusion-active conformation. In an effort to discover small organic inhibitors that block gp41 activation, we have generated a biased combinatorial chemical library of non-natural binding elements targeted to the gp41 core. From this library of 61,275 potential ligands, we have identified elements that, when covalently attached to a peptide derived from the gp41 outer-layer alpha-helix, contribute to the formation of a stable complex with the inner core and to inhibition of gp41-mediated cell fusion.
- Publication
Nature structural biology, 1999, Vol 6, Issue 10, p953
- ISSN
1072-8368
- Publication type
Journal Article
- DOI
10.1038/13324