RAPID resistance to BET inhibitors is mediated by FGFR1 in glioblastoma

• Published in: Scientific reports Vol. 14; no. 1; p. 9284
• Main Authors: Jermakowicz, Anna M., Kurimchak, Alison M., Johnson, Katherine J., Bourgain-Guglielmetti, Florence, Kaeppeli, Simon, Affer, Maurizio, Pradhyumnan, Hari, Suter, Robert K., Walters, Winston, Cepero, Maria, Duncan, James S., Ayad, Nagi G.
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 23.04.2024; Nature Publishing Group; Nature Portfolio
• Subjects: 631/45/275; 631/67/1922; Animals; Brain Neoplasms - drug therapy; Brain Neoplasms - metabolism; Brain Neoplasms - pathology; Brain tumors; Bromodomain Containing Proteins; Cell Line, Tumor; Cell proliferation; Cell Proliferation - drug effects; Clinical trials; Drug Resistance, Neoplasm - drug effects; Fibroblast growth factor receptor 1; Glioblastoma; Glioblastoma - drug therapy; Glioblastoma - genetics; Glioblastoma - metabolism; Glioblastoma - pathology; Glioma; Humanities and Social Sciences; Humans; Inhibitors; Mass spectrometry; Mass spectroscopy; Mice; multidisciplinary; Proteins; Proteins - antagonists & inhibitors; Proteins - metabolism; Proteomics; Proteomics - methods; Receptor, Fibroblast Growth Factor, Type 1 - antagonists & inhibitors; Receptor, Fibroblast Growth Factor, Type 1 - genetics; Receptor, Fibroblast Growth Factor, Type 1 - metabolism; Science; Science (multidisciplinary); Temporal variations; Therapeutic targets; Xenograft Model Antitumor Assays

Bromodomain and extra-terminal domain (BET) proteins are therapeutic targets in several cancers including the most common malignant adult brain tumor glioblastoma (GBM). Multiple small molecule inhibitors of BET proteins have been utilized in preclinical and clinical studies. Unfortunately, BET inhi...