000125914 001__ 125914
000125914 005__ 20240731103333.0
000125914 0247_ $$2doi$$a10.3390/cells12040653
000125914 0248_ $$2sideral$$a133425
000125914 037__ $$aART-2023-133425
000125914 041__ $$aeng
000125914 100__ $$aKampa, Marilena
000125914 245__ $$aPromising perspectives of the antiproliferative GPER inverse agonist ERa17p in breast cancer
000125914 260__ $$c2023
000125914 5060_ $$aAccess copy available to the general public$$fUnrestricted
000125914 5203_ $$aThe estrogen receptor α (ERα) corresponds to a large platform in charge of the recruitment of a panel of molecules, including steroids and related heterocyclic derivatives, oligonucleotides, peptides and proteins. Its 295–311 region is particularly targeted by post-translational modifications, suggesting that it could be crucial for the control of transcription. In addition to anionic phospholipids, the ERα 295–311 fragment interacts with Ca2+-calmodulin, the heat shock protein 70 (Hsp70), ERα and possibly importins. More recently, we have demonstrated that it is prone to interacting with the G-protein-coupled estrogen receptor (GPER). In light of these observations, the pharmacological profile of the corresponding peptide, namely ERα17p, has been explored in breast cancer cells. Remarkably, it exerts apoptosis through GPER and induces a significant decrease (more than 50%) of the size of triple-negative breast tumor xenografts in mice. Herein, we highlight not only the promising therapeutic perspectives in the use of the first peptidic GPER modulator ERα17p, but also the opportunity to modulate GPER for clinical purposes.
000125914 540__ $$9info:eu-repo/semantics/openAccess$$aby$$uhttp://creativecommons.org/licenses/by/3.0/es/
000125914 590__ $$a5.1$$b2023
000125914 592__ $$a1.547$$b2023
000125914 591__ $$aCELL BIOLOGY$$b63 / 205 = 0.307$$c2023$$dQ2$$eT1
000125914 593__ $$aBiochemistry, Genetics and Molecular Biology (miscellaneous)$$c2023$$dQ1
000125914 594__ $$a9.9$$b2023
000125914 655_4 $$ainfo:eu-repo/semantics/article$$vinfo:eu-repo/semantics/publishedVersion
000125914 700__ $$aLappano, Rosamaria
000125914 700__ $$aGrande, Fedora
000125914 700__ $$aRizzuti, Bruno
000125914 700__ $$aMaggiolini, Marcello
000125914 700__ $$aCastanas, Elias
000125914 700__ $$aJacquot, Yves
000125914 773__ $$g12, 4 (2023), 653 [12 pp.]$$pCells$$tCells$$x2073-4409
000125914 8564_ $$s1084311$$uhttps://zaguan.unizar.es/record/125914/files/texto_completo.pdf$$yVersión publicada
000125914 8564_ $$s2676304$$uhttps://zaguan.unizar.es/record/125914/files/texto_completo.jpg?subformat=icon$$xicon$$yVersión publicada
000125914 909CO $$ooai:zaguan.unizar.es:125914$$particulos$$pdriver
000125914 951__ $$a2024-07-31-09:47:08
000125914 980__ $$aARTICLE