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Products
Pharmacology
Type
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- Technical support
- Resources
ERα17p
Cat. No. GE-010
Structure:
H-Pro-Leu-Met-Ile-Lys-Arg-Ser-Lys-Lys-Asn-Ser-Leu-Ala-Leu-Ser-Leu-Thr-OH
Other Names:
ERα 295-311
Activity:
GPER inverse agonist
ERα17p is a GPER inverse agonist, corresponding to residues 295-311 of the human estrogen receptor α (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 ERα9, as well as associating 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.
Mallet et al (2021) The Antitumor Peptide ERα17p Exerts Anti-Hyperalgesic and Anti-Inflammatory Actions Through GPER in Mice. Front Endocrinol. 12 578250 PMID: 33815268
Jouffre et al (2023) Identification of a human estrogen receptor α tetrapeptidic fragment with dual antiproliferative and anti-nociceptive action. Sci Rep. 13(1) 1326 PMID: 36693877
Kampa et al (2023) Promising Perspectives of the Antiproliferative GPER Inverse Agonist ERα17p in Breast Cancer. Cells 12(4) 653 PMID: 36831322
Related areas
All peptides >
All G protein-coupled estrogen receptor modulators >
All cancer research categories >
Technical Data
| Structure | H-Pro-Leu-Met-Ile-Lys-Arg-Ser-Lys-Lys-Asn-Ser-Leu-Ala-Leu-Ser-Leu-Thr-OH |
| Molecular Weight | 1899.13 |
| Formula | C84H154N24O23S |
| Sequence | PLMIKRSKKNSLALSLT |
| Modifications | None |
Solubility and Storage
| Solubility | Soluble in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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