EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor
Eva De Mol
1
,
R Bryn Fenwick
1
,
Christopher T W Phang
1
,
Víctor Buzón
2
,
Elżbieta Szulc
1
,
Alex De La Fuente
1
,
Albert Escobedo
1
,
Jesús García
1
,
Carlos W. Bertoncini
1
,
Eva Estébanez-Perpiñá
2
,
Iain McEwan
3
,
A. Riera
1, 4
,
Xavier Salvatella
1, 5
1
Publication type: Journal Article
Publication date: 2016-07-14
scimago Q1
wos Q2
SJR: 1.383
CiteScore: 7.1
Impact factor: 3.8
ISSN: 15548929, 15548937
PubMed ID:
27356095
Biochemistry
General Medicine
Molecular Medicine
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.
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131
Total citations:
131
Citations from 2024:
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(25.19%)
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MLA
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GOST
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De Mol E. et al. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor // ACS Chemical Biology. 2016. Vol. 11. No. 9. pp. 2499-2505.
GOST all authors (up to 50)
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De Mol E., Fenwick R. B., Phang C. T. W., Buzón V., Szulc E., De La Fuente A., Escobedo A., García J., Bertoncini C. W., Estébanez-Perpiñá E., McEwan I., Riera A., Salvatella X. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor // ACS Chemical Biology. 2016. Vol. 11. No. 9. pp. 2499-2505.
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TY - JOUR
DO - 10.1021/acschembio.6b00182
UR - https://doi.org/10.1021/acschembio.6b00182
TI - EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor
T2 - ACS Chemical Biology
AU - De Mol, Eva
AU - Fenwick, R Bryn
AU - Phang, Christopher T W
AU - Buzón, Víctor
AU - Szulc, Elżbieta
AU - De La Fuente, Alex
AU - Escobedo, Albert
AU - García, Jesús
AU - Bertoncini, Carlos W.
AU - Estébanez-Perpiñá, Eva
AU - McEwan, Iain
AU - Riera, A.
AU - Salvatella, Xavier
PY - 2016
DA - 2016/07/14
PB - American Chemical Society (ACS)
SP - 2499-2505
IS - 9
VL - 11
PMID - 27356095
SN - 1554-8929
SN - 1554-8937
ER -
Cite this
BibTex (up to 50 authors)
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@article{2016_De Mol,
author = {Eva De Mol and R Bryn Fenwick and Christopher T W Phang and Víctor Buzón and Elżbieta Szulc and Alex De La Fuente and Albert Escobedo and Jesús García and Carlos W. Bertoncini and Eva Estébanez-Perpiñá and Iain McEwan and A. Riera and Xavier Salvatella},
title = {EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor},
journal = {ACS Chemical Biology},
year = {2016},
volume = {11},
publisher = {American Chemical Society (ACS)},
month = {jul},
url = {https://doi.org/10.1021/acschembio.6b00182},
number = {9},
pages = {2499--2505},
doi = {10.1021/acschembio.6b00182}
}
Cite this
MLA
Copy
De Mol, Eva, et al. “EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor.” ACS Chemical Biology, vol. 11, no. 9, Jul. 2016, pp. 2499-2505. https://doi.org/10.1021/acschembio.6b00182.