EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor
| العنوان: | EPI-001, a compound active against castration-resistant prostate cancer, targets transactivation unit 5 of the androgen receptor |
|---|---|
| المؤلفون: | R. Bryn Fenwick, Elzbieta Szulc, Antoni Riera, Alex de la Fuente, Carlos W. Bertoncini, Christopher T. W. Phang, Xavier Salvatella, Iain J. McEwan, Victor Buzon, Jesús García, Eva Estébanez-Perpiñá, Albert Escobedo, Eva De Mol |
| المساهمون: | Universitat de Barcelona |
| المصدر: | Dipòsit Digital de la UB Universidad de Barcelona Recercat. Dipósit de la Recerca de Catalunya instname CONICET Digital (CONICET) Consejo Nacional de Investigaciones Científicas y Técnicas instacron:CONICET ACS Chemical Biology |
| بيانات النشر: | American Chemical Society, 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | 0301 basic medicine, Male, Transcriptional Activation, medicine.medical_specialty, CIENCIAS MÉDICAS Y DE LA SALUD, Nuclear Magnetic Resonance, Otras Ciencias Biológicas, Nuclear receptors (Biochemistry), Biochemistry, Article, Biotecnología de la Salud, Androgen deprivation therapy, purl.org/becyt/ford/1 [https], Ciencias Biológicas, 03 medical and health sciences, chemistry.chemical_compound, Transactivation, Prostate cancer, Internal medicine, Chemical Biology, medicine, Humans, EPI-001, Androgen Receptor Antagonists, purl.org/becyt/ford/3.4 [https], Benzhydryl Compounds, Receptor, purl.org/becyt/ford/1.6 [https], Càncer de pròstata, Prostatic Neoplasms, General Medicine, medicine.disease, 3. Good health, Androgen receptor, Structure-based drug discovery, 030104 developmental biology, Endocrinology, chemistry, Nuclear receptor, Receptors, Androgen, Receptors nuclears (Bioquímica), Cancer research, Molecular Medicine, purl.org/becyt/ford/3 [https], Chlorohydrins, Orchiectomy, CIENCIAS NATURALES Y EXACTAS, Otras Biotecnologías de la Salud |
| الوصف: | 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. Fil: de Mol, Eva. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Fenwick, R. Bryn. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Phang, Christopher T. W.. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Buzón, Victor. Universidad de Barcelona; España Fil: Szulc, Elzbieta. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: de la Fuente, Alex. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Escobedo, Albert. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: García, Jesús. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Bertoncini, Carlos Walter. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Biología Molecular y Celular de Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Biología Molecular y Celular de Rosario; Argentina. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España Fil: Estébanez Perpiñá, Eva. Universidad de Barcelona; España Fil: McEwan, Iain J.. University of Aberdeen; Reino Unido Fil: Riera, Antoni. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España. Universidad de Barcelona; España Fil: Salvatella, Xavier. Barcelona Institute of Science and Technology. Institute for Research in Biomedicine; España. Institució Catalana de Recerca i Estudis Avancats; España |
| وصف الملف: | application/pdf |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bd9aadb8d704c5e1510cf3d4375f543 http://hdl.handle.net/2445/102449 |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....8bd9aadb8d704c5e1510cf3d4375f543 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |