Androgen receptor (AR) is a transcription factor and validated therapeutic target for prostate cancer. All currently approved inhibitors of AR target its folded C-terminus ligand-binding domain. Resistance to these therapies is mediated by expression of constitutively active splice variants of AR that are truncated and lack LBD. Thus targeting the intrinsically disordered N-terminal domain of AR provides a novel therapeutic mechanism. Here we report our approach to the discovery and clinical development of small molecule inhibitors of this drug target previously considered to be “un-druggable”.

Development of drugs that directly target the intrinsically disordered region of N-terminal domain of androgen receptor

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.