| Autor: |
Eugenio Morelli, Zachary R. Hunter, Mariateresa Fulciniti, Annamaria Gullà, Ida Daniela Perrotta, Valeria Zuccalà, Cinzia Federico, Giada Juli, Martina Manzoni, Domenica Ronchetti, Enrica Romeo, Maria Eugenia Gallo Cantafio, Debora Soncini, Lorenza Maltese, Marco Rossi, Aldo M. Roccaro, Michele Cea, Pierfrancesco Tassone, Antonino Neri, Steven C. Treon, Nikhil C. Munshi, Giuseppe Viglietto, Nicola Amodio |
| Jazyk: |
angličtina |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
Experimental Hematology & Oncology, Vol 11, Iss 1, Pp 1-6 (2022) |
| Druh dokumentu: |
article |
| ISSN: |
2162-3619 |
| DOI: |
10.1186/s40164-022-00305-x |
| Popis: |
Abstract Activating G protein-coupled estrogen receptor 1 (GPER1) is an attractive therapeutic strategy for treating a variety of human diseases including cancer. Here, we show that GPER1 is significantly upregulated in tumor cells from different cohorts of Waldenström Macroglobulinemia (WM) patients compared to normal B cells. Using the clinically applicable GPER1-selective small-molecule agonist G-1 (also named Tespria), we found that pharmacological activation of GPER1 leads to G2/M cell cycle arrest and apoptosis both in vitro and in vivo in animal models, even in the context of the protective bone marrow milieu. Activation of GPER1 triggered the TP53 pathway, which remains actionable during WM progression. Thus, this study identifies a novel therapeutic target in WM and paves the way for the clinical development of the GPER1 agonist G-1. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
|
|
Nepřihlášeným uživatelům se plný text nezobrazuje |
K zobrazení výsledku je třeba se přihlásit.
|
