CREBBP/EP300 Bromodomain Inhibition Affects the Proliferation of AR-Positive Breast Cancer Cell Lines

• Published in: Molecular cancer research Vol. 17; no. 3; pp. 720 - 730
• Main Authors: Garcia-Carpizo, Veronica, Ruiz-Llorente, Sergio, Sarmentero, Jacinto, González-Corpas, Ana, Barrero, Maria J
• Format: Journal Article
• Language: English
• Published: United States 01.03.2019
• Subjects: Androgens - pharmacology; Azepines - pharmacology; Benzimidazoles - pharmacology; Breast Neoplasms - drug therapy; Breast Neoplasms - genetics; Breast Neoplasms - metabolism; Breast Neoplasms - pathology; Cell Line, Tumor; Cell Proliferation - drug effects; Cell Proliferation - physiology; CREB-Binding Protein - antagonists & inhibitors; Down-Regulation - drug effects; E1A-Associated p300 Protein - antagonists & inhibitors; Female; Gene Expression Regulation, Neoplastic - drug effects; Humans; Isoxazoles - pharmacology; Protein Domains; Receptors, Androgen - genetics; Receptors, Androgen - metabolism; Triazoles - pharmacology

Inhibitors that prevent the binding of bromodomains to acetylated histones hold therapeutic potential. However, the effects of targeting most of the 60 different bromodomains found in the human proteome remain unexplored. Here, we investigate the molecular mechanisms responsible for the antiprolifer...