Please note: this product can only be supplied to registered research and development facilities, and may be used for in vitro research use only, not for administration to humans or animals.

GPER inverse agonist.

ERα17p is a GPER inverse agonist, corresponding to residues 295-311 of the human estrogen receptor  (ERα). ? This 295-311 region is targeted by post-translational modifications and is involved in the recruitment of Ca2+-calmodulin, Hsp70 and the ubiquitin-protein isopeptide ligase E6-associated protein (E6AP), an E3 ligase catalyzing the ubiquitination of ER9, as well as association with ERα. ERα17p triggers membrane-initiated pro-apoptotic events in both ERα-positive and -negative breast cancer cell lines with a preference for ERα-positive cancer cells, and induces a decrease of more than 50% of the size of triple-negative breast tumour xenografts. ERα17p also exerts GPER mediated anti-hyperalgesic and anti-inflammatory actions in mice.

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