2. Academic Validation
  3. EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor

EPI-001, A Compound Active against Castration-Resistant Prostate Cancer, Targets Transactivation Unit 5 of the Androgen Receptor

  • ACS Chem Biol. 2016 Sep 16;11(9):2499-505. doi: 10.1021/acschembio.6b00182.
Eva De Mol 1,  R Bryn Fenwick 1,  Christopher T W Phang 1,  Victor Buzón 2,  Elzbieta Szulc 1,  Alex de la Fuente 1,  Albert Escobedo 1,  Jesús García 1,  Carlos W Bertoncini 1,  Eva Estébanez-Perpiñá 2,  Iain J McEwan 3,  Antoni Riera 1 4,  Xavier Salvatella 1 5
Affiliations

Affiliations

  • 1 Institute for Research in Biomedicine (IRB Barcelona), The Barcelona Institute of Science and Technology , Baldiri Reixac 10, 08028 Barcelona, Spain.
  • 2 Departament de Bioquímica i Biología Molecular, and Institute of Biomedicine, University of Barcelona (IBUB) , Baldiri Reixac 10, 08028 Barcelona, Spain.
  • 3 Institute of Medical Sciences, School of Medicine, Medical Sciences and Nutrition, University of Aberdeen , IMS Building, Foresterhill, Aberdeen AB25 2ZD, Scotland , United Kingdom.
  • 4 Departament de Química Orgànica, Universitat de Barcelona , Martí i Franqués 1-11, 08028 Barcelona, Spain.
  • 5 ICREA, Passeig Lluís Companys 23 , 08010 Barcelona, Spain.
PMID: 27356095 DOI: 10.1021/acschembio.6b00182
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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