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. Author manuscript; available in PMC: 2008 Aug 21.

Published in final edited form as: J Comb Chem. 2007 May 27;9(4):592–600. doi: 10.1021/cc070023a

Cellular activities of OxDex-BHK1-6 (see Figure S3 for structures). (A) Cartoon of the assay employed to measure the AD-like activity of the peptoid (see text for details). TC = transcription complex. (B) HeLa cell permeability of the OxDex-peptoid conjugates. OxDex-AEEA-CONH₂ (×), OxDex-BHK1 ( ), OxDex-BHK2( ), OxDex-BHK3( ), OxDex-BHK4( ), OxDex-BHK5( ) or OxDex-BHK6( ). This assay³¹ is almost identical to that shown in A, except that the Gal4 fusion protein also contains a VP16 AD. The values shown are ratios of the level of induction measured using dual-luciferase assay system (Promega; Gal4-responsive/constitutive). Data points for OxDex-BHK1 and OxDex-BHK3 at 100 μM could not be obtained due to significant cytotoxicity at this concentration. (C) Activation domain-like activity of OxDex-BHK1-6 in the assay shown schematically in (A). The symbol designations are the same as in (B). The data, shown as the mean + SD or mean - SD, are representative of at least three independent experiments with each point measured in duplicate. The curves are the best fit of the data to the sigmoidal dose-response model in Prism4.0.

Inline graphic — Cellular activities of OxDex-BHK1-6 (see Figure S3 for structures). (A) Cartoon of the assay employed to measure the AD-like activity of the peptoid (see text for details). TC = transcription complex. (B) HeLa cell permeability of the OxDex-peptoid conjugates. OxDex-AEEA-CONH₂ (×), OxDex-BHK1 ( ), OxDex-BHK2( ), OxDex-BHK3( ), OxDex-BHK4( ), OxDex-BHK5( ) or OxDex-BHK6( ). This assay³¹ is almost identical to that shown in A, except that the Gal4 fusion protein also contains a VP16 AD. The values shown are ratios of the level of induction measured using dual-luciferase assay system (Promega; Gal4-responsive/constitutive). Data points for OxDex-BHK1 and OxDex-BHK3 at 100 μM could not be obtained due to significant cytotoxicity at this concentration. (C) Activation domain-like activity of OxDex-BHK1-6 in the assay shown schematically in (A). The symbol designations are the same as in (B). The data, shown as the mean + SD or mean - SD, are representative of at least three independent experiments with each point measured in duplicate. The curves are the best fit of the data to the sigmoidal dose-response model in Prism4.0.