stERAP

stERAP (stapled estrogen receptor alpha activity regulator synthetic peptide) is a cell-permeable, hydrocarbon-stapled peptide developed by researchers at Tokushima University. It is designed to specifically disrupt the protein-protein interaction between Brefeldin A-Inhibited Guanine nucleotide-exchange protein 3 (BIG3) and the tumor suppressor prohibitin-2 (PHB2). In many breast cancers and osteosarcomas, overexpressed BIG3 binds to and sequesters PHB2, inactivating its tumor-suppressive functions. By binding to PHB2, stERAP prevents the BIG3-PHB2 interaction, releasing PHB2 to translocate into the nucleus where it acts as a transcriptional co-repressor of estrogen receptor alpha (ERα). This suppresses both genomic and non-genomic ERα activation, leading to significant anti-tumor effects. stERAP has shown preclinical efficacy in models of luminal-type breast cancer, HER2-overexpressing breast cancer (including trastuzumab-resistant breast cancer), triple-negative breast cancer, and osteosarcoma.

Other names

stapled ERAPstapled estrogen receptor alpha activity regulator synthetic peptide