Two ERs/GPER-targeting PROTACs (UI-EP001 and UI-EP002) have been designed, which effectively degrade ERα, ERβ, and GPER, inducing cytotoxicity and G2/M cell cycle arrest in MCF-7 (ERα+/ERβ+/GPER+) and SKBR3 (ERα−/ERβ−/GPER+) BC cells but not in MDA-MB-231 BC cells that do not express functional ERα/ERβ/GPER.55 The gene discussed is GPER1; the disease is breast cancer.