Figure 1
From: Stapled BIG3 helical peptide ERAP potentiates anti-tumour activity for breast cancer therapeutics
Stapled ERAP has sustained stability and highly sensitive capacity to inhibit the BIG3-PHB2 interaction. (a) Primary structures for ERAP and its stapled analogs. (b,c) An MTT assay evaluating the inhibitory effects of stapled ERAPs on the growth of 10 nM E2-dependent MCF-7 cells (b) and of mammary epithelial MCF-10A cells (c). Cells were given a single treatment at 0 h. These data represent the mean ± s.d. of three independent experiments (**P < 0.01 and ***P < 0.001 via two-sided Student’s t-tests). (d) The inhibitory effects of stapled ERAP treatment on BIG3-PHB2 interactions in MCF-7 cells. ERAP was used as a positive control for the inhibition of the BIG3-PHB2 interaction. (e) In vitro direct interaction of stapled ERAPs (stERAP-1 and -2) and recombinant PHB2 discerned by surface plasmon resonance systems. (f) CD spectra and α-helical content of ERAP and stERAP analogs (stERAP-1 and -2) in 10 mM sodium phosphate buffer (pH 7.0).
