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Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive ?-helix mimetic library.

ABSTRACT: The evaluation of a comprehensive ?-helix mimetic library for binding the gp41 NHR hydrophobic pocket recognizing an intramolecular CHR ?-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 ?M) 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 ?M).

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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