Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/102449
Title: | EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor |
Author: | Mol, Eva de Fenwick, R. Bryn Phang, Christopher T. W. Buzón Redorta, Víctor Szulc, Elzbieta Maria Fuente Cebrián, Àlex de la Escobedo Pascual, Albert García Arroyo, Jesús Bertoncini, Carlos W. Estébanez Perpiñá, Eva McEwan, Iain J. Riera i Escalé, Antoni Salvatella i Giralt, Xavier |
Keywords: | Càncer de pròstata Receptors nuclears (Bioquímica) Prostate cancer Nuclear receptors (Biochemistry) |
Issue Date: | 29-Jun-2016 |
Publisher: | American Chemical Society |
Abstract: | Castration-resistant prostate cancer is the lethal condition suffered by prostate cancer patients that become refractory to androgen deprivation therapy. EPI-001 is a recently identified compound active against this condition that modulates the activity of the androgen receptor, a nuclear receptor that is essential for disease progression. The mechanism by which this compound exerts its inhibitory activity is however not yet fully understood. Here we show, by using high resolution solution nuclear magnetic resonance spectroscopy, that EPI-001 selectively interacts with a partially folded region of the transactivation domain of the androgen receptor, known as transactivation unit 5, that is key for the ability of prostate cells to proliferate in the absence of androgens, a distinctive feature of castration-resistant prostate cancer. Our results can contribute to the development of more potent and less toxic novel androgen receptor antagonists for treating this disease. |
Note: | Versió postprint del document publicat a: http://dx.doi.org/10.1021/acschembio.6b00182 |
It is part of: | ACS Chemical Biology, 2016, vol. 11, num. 9, p. 2499-2505 |
URI: | http://hdl.handle.net/2445/102449 |
Related resource: | http://dx.doi.org/10.1021/acschembio.6b00182 |
ISSN: | 1554-8929 |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) Articles publicats en revistes (Bioquímica i Biomedicina Molecular) Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona)) Publicacions de projectes de recerca finançats per la UE |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
662965.pdf | 244.78 kB | Adobe PDF | View/Open |
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.