Searchable abstracts of presentations at key conferences in endocrinology

ea0042p2 | (1) | Androgens2016

Functional analysis of the AR LBD dimerization surface

Helsen Christine , Prekovic Stefan , van Royen Martin E , Houtsmuller Adriaan B , Fuentes-Prior Pablo , Estebanez-Perpina Eva , Claessens Frank

The androgen receptor (AR) is a multidomain transcription factor consisting of an aminoterminal domain (NTD), a DNA binding domain (DBD) and a ligand binding domain (LBD). Binding of androgens marks the start of a sequence of intra- and interdomain communications, DNA binding, coregulator recruitment and gene activation. Besides the DBD-mediated dimerization on the DNA, there is a functionally relevant N/C interaction. The contribution of the intra- and intermolecular N/C inte...

ea0042oc16 | (1) | Androgens2016

Genomic analysis of Enzalutamide-resistant cells

Prekovic Stefan , Van den Broeck Thomas , Smeets Elien , van Royen Martin , Houtsmuller Adriaan , Sahu Biswajyoti , Pihlajamaa Paivi , Janne Olli A. , Attard Gerhardt , Claessens Frank , Helsen Christine

Enzalutamide (Enza) is a second-generation antiandrogen currently used in the clinic for treatment of metastatic prostate cancer. It significantly prolonged survival of men with metastatic castration resistant prostate cancer after chemotherapy by a median of 4.8 months in comparison to the placebo group. However, in a subset of patientÂ’s beneficial effect of Enza cannot be observed, while others who initially respond eventually develop resistance towards the treatment. U...

ea0071001 | Dimerization of the ligand-binding domain is crucial for proper functioning of the androgen receptor | BES2020

Dimerization of the ligand-binding domain is crucial for proper functioning of the androgen receptor

Sarah El Kharraz , Christine Helsen , Vanessa Dubois , Florian Handle , Claude Libert , Martin Van Royen , Adriaan Houtsmuller , Claes Ohlsson , Matti Poutanen , Nina Atanassova , Ekaterina Pavlova , Dirk Vanderschueren , Frank Claessens

The importance of the androgen receptor (AR) in the development and maintenance of the male phenotype is demonstrated by patients with androgen insensitivity syndrome (AIS). These patients carry germline mutations in the AR and display a mild to complete intersex phenotype. The AR belongs to the subfamily of steroid receptors, which need to form homodimers to execute their role as transcription factors. For estrogen receptors, dimerization via the DNA-binding domains as well a...