Miniatura

Fitxers

662965.pdf (244.78 KB)

Tipus de document

Article

Versió

Versió acceptada

Data de publicació

2016-06-29

Tots els drets reservats

Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/102449

EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor

Títol de la revista

Autors

Director/Tutor

ISSN de la revista

Títol del volum

Recurs relacionat

http://dx.doi.org/10.1021/acschembio.6b00182

Resum

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.

Matèries

Càncer de pròstata, Receptors nuclears (Bioquímica)

Matèries (anglès)

Prostate cancer, Nuclear receptors (Biochemistry)

Citació

Col·leccions

Articles publicats en revistes (Bioquímica i Biomedicina Molecular)
<b>Publicacions de projectes de recerca finançats per la UE</b>
Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona))
Articles publicats en revistes (Química Inorgànica i Orgànica)

Citació

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. EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor. _ACS Chemical Biology_. 2016. Vol. 11, núm. 9, pàgs. 2499-2505. [consulta: 24 de gener de 2026]. ISSN: 1554-8929. [Disponible a: https://hdl.handle.net/2445/102449]

Exportar metadades

JSON - METS

Compartir registre