Seminar Series

IDP Conversations

Date and Time

07 July 2021
11AM (EDT) / 5PM (CEST)

Session Link

The seminar series will be recorded and may be shared for later viewing.

Past Sessions

New Equilibrium presents IDP Conversations, a monthly seminar series focused on intrinsically disordered proteins (IDPs). Our goal is to foster a multi-perspective discussion on modeling and targeting IDPs. Each seminar, featuring speakers across academia and industry, includes a 40-minute presentation followed by a conversation.

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

Androgen receptor is a transcription factor and validated therapeutic target for prostate cancer. All currently approved inhibitors of androgen receptor target its folded C-terminus ligand-binding domain. Resistance to these therapies is mediated by expression of constitutively active splice variants of androgen receptor that are truncated and lack a ligand-binding domain. Thus targeting the intrinsically disordered N-terminal domain of androgen receptor 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”.

Speaker: Marianne Sadar, Ph.D.

Dr. Sadar is a Professor of Pathology and Laboratory Medicine at the University of British
Columbia and Distinguished Scientist in the Department of Genome Sciences at BC Cancer. Dr.
Sadar’s research has focused on identifying mechanisms of transactivating the androgen receptor
which is a therapeutic target for prostate cancer and other diseases. Uniquely her research has
focused on developing therapies to the intrinsically disordered N-terminal domain of the
androgen receptor which acts as a hub for essential protein-protein interactions required for its
transcriptional activity. She has identified the first small molecule inhibitors that directly bind to
the N-terminal domain of androgen receptor that has yielded compounds that have been taken
into clinical trials. Her first-in-class compounds were granted a new stem class from the USAN
council “-aniten”. Related work includes developing imaging agents with small molecules that
bind to unique regions of the N-terminal domain of androgen receptor. Her current areas of
research interest are concentrated predominantly on indications for prostate cancer and breast
. Dr. Sadar is a co-founder, and past Director and Officer of ESSA Pharma Inc. (EPIX,
NASDAQ). She has served in leadership positions such as President of the Society of Basic
Urologic Research and the Y2017 Chair of the USA Army’s Department of Defence’s
Programmatic Panel for their Prostate Cancer Research Program. Dr. Sadar has served on over
50 grant panels including 5 years on the NIH study session for Drug Discovery &
Molecular Pharmacology.

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