Figure 3
From: Stapled BIG3 helical peptide ERAP potentiates anti-tumour activity for breast cancer therapeutics
StERAP-6 has in vivo anti-tumour efficacy in xenograft models of human ERα-positive breast cancer. (a) Tumour growth assessed after daily (left) or every 4 days (right) intraperitoneal injection of 1.4 and 14 mg kg−1 stERAP-6 or unstapled original ERAP (ERAP) in KPL-3C xenograft mice. The tumour sizes represent the mean ± s.e.m. of each group (n = 5). (b) Immunoblot analysis of the binding inhibition of the BIG3-PHB2 interaction in tumours treated intraperitoneally with daily (left) or every 4 days (right) of stERAP-6 or ERAP. (c) The inhibitory effects of stERAP-6 or ERAP on ERα-target genes expression in tumours treated for 28 days. The results were expressed as the fold increase over untreated tumours (set at 1.0). NS: no significance. The data represent the mean ± s.e.m. of five independent tumours. (d) Immunoblot analysis of the phosphorylation levels of Akt and MAPK in tumours treated intraperitoneally with daily (left) or every 4 days (right) of stERAP-6 or unstapled original (ERAP). (e) Tumour growth by intravenous injection of stERAP-6 daily (left) or weekly (right) in KPL-3C orthotropic breast cancer xenograft mice. The tumour sizes represent the mean ± s.e.m. of each group (n = 5). *P < 0.05, **P < 0.01, and ***P < 0.001 via two-sided Student’s t-tests.
