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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, Victor
Szulc, Elzbieta
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:
It is part of: ACS Chemical Biology, 2016, vol. 11, num. 9, p. 2499-2505
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ISSN: 1554-8929
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)
Articles publicats en revistes (Institut de Recerca Biomèdica (IRB Barcelona))
Articles publicats en revistes (Bioquímica i Biomedicina Molecular)

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