Figure 2
From: Stapled BIG3 helical peptide ERAP potentiates anti-tumour activity for breast cancer therapeutics
Stapled ERAP without olefin metathesis suppresses the E2-dependent responsiveness with long-term stability. (a) Primary structures for stapled ERAP (stERAP-6) without olefin. (b) CD spectra and α-helical content of stERAP-6. (c) An MTT assay evaluating the duration of the inhibitory effects of stERAP-6 on the growth of 10 nM E2-dependent MCF-7 cells (left) and of mammary epithelial MCF-10A cells (right). Cells were given a single treatment at 0 h. These data represent the mean ± s.d. of three independent experiments. (d) The inhibitory effects of stERAP-6 on BIG3-PHB2 interactions in MCF-7 cells. (e) The duration of the inhibitory effects of stERAP-6 on ERα-target genes expression in MCF-7 cells for the times indicated. The results were expressed as the fold increase over untreated cells at 24 h (set at 1.0). The data represent the mean ± s.e.m. of three independent experiments. (f) Representative immunofluorescence images of the subcellular localization of HA-tagged stERAP-6 (HA-stERAP-6; green) and PHB2 (red) in the presence of E2. *P < 0.05, **P < 0.01, and ***P < 0.001 via two-sided Student’s t-tests.
