Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive ?-helix mimetic library.
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ABSTRACT:
SUBMITTER: Whitby LR
PROVIDER: S-EPMC3321071 | biostudies-literature | 2012 Apr
REPOSITORIES: biostudies-literature
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Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.
Whitby Landon R LR Boyle Kristopher E KE Cai Lifeng L Yu Xiaoqian X Gochin Miriam M Boger Dale L DL
Bioorganic & medicinal chemistry letters 20120303 8
The evaluation of a comprehensive α-helix mimetic library for binding the gp41 NHR hydrophobic pocket recognizing an intramolecular CHR α-helix provided a detailed depiction of structural features required for binding and led to the discovery of small molecule inhibitors (K(i) 0.6-1.3 μM) that not only match or exceed the potency of those disclosed over the past decade, but that also exhibit effective activity in a cell-cell fusion assay (IC(50) 5-8 μM). ...[more]
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