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EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor
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
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.
Càncer de pròstata
Receptors nuclears (Bioquímica)
Prostate cancer
Nuclear receptors (Biochemistry)
(c) American Chemical Society , 2016
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American Chemical Society
         

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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
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
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